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Background: Diabetes mellitus is a chronic metabolic disorder, characterized by hyperglycemia over a prolonged period, disturbance of fat, protein and carbohydrate metabolism, resulting from defective insulin secretion, insulin action or both. Dipeptidyl peptidase-IV (DPP-IV) inhibitors are relatively a new class of oral hypoglycemic agents that reduces the deterioration of gut-derived endogenous incretin hormones that are secreted in response to food ingestion to stimulate the secretion of insulin from beta cells of pancreas. Objective: In this study, synthesis, characterization, and biological assessment of twelve novel phenanthridine sulfonamide derivatives 3a-3l as potential DPP-IV inhibitors was carried out. The target compounds were docked to study the molecular interactions and binding affinities against DPP-IV enzyme. Methods: The synthesized molecules were characterized using 1H-NMR, 13C-NMR, IR, and MS. Quantum-polarized ligand docking (QPLD) was also performed. Results: In vitro biological evaluation of compounds 3a-3l reveals comparable DPP-IV inhibitory activities ranging from 10%-46% at 100 µM concentration, where compound 3d harboring ortho-fluoro moiety exhibited the highest inhibitory activity. QPLD study shows that compounds 3a-3l accommodate DPP-IV binding site and form H-bonding with the R125, E205, E206, S209, F357, R358, K554, W629, S630, Y631, Y662, R669 and Y752 backbones. Conclusion: In conclusion, phenanthridine sulfonamides could serve as potential DPP-IV inhibitors that require further structural optimization in order to enhance their inhibitory activity.

Ovarian cancer is one of the most common gynecological malignancies. Due to the absence of effective screening methods, ovarian cancer is usually diagnosed at late stages. Patients with pathogenic and likely-pathogenic germline variants (PGVs) in BRCA1 or BRCA2 harbor elevated risk of developing both ovarian and breast cancers. Identifying PGVs may help in both cancer prevention and active disease treatment. Worldwide prevalence of PGVs varies and the matter is poorly addressed among Arab patients.Patients with epithelial ovarian, fallopian tube or primary peritoneal cancers were offered the universal 20 or 84-multi-gene panel testing as per standard guidelines. Cascade family screening was also offered to all first and second-degree relatives of PGV positive patients. Genetic testing was done at a referral lab using a next generation sequencing (NGS)-based platform.During the study period, 152 patients, median age (range): 50 (18-79) years old, were tested. The majority (n = 100, 65.8%) had high-grade serous carcinoma, and 106 patients (69.7%) had metastatic disease at presentation. In total, 38 (25.0%) had PGVs, while 47 (30.9%) others had variants of uncertain significance (VUS). PGVs were mostly in BRCA1 (n = 21, 13.8%) and in BRCA2 (n = 12, 7.9%), while 6 (3.9%) others had PGVs in non-BRCA1/2 genes. PGV rates were significantly higher among 15 patients with a positive family history of ovarian cancer (60.0%, p = .022) and among 52 patients with a positive family history of breast cancer (40.4%, p = .017).PGVs are common among Jordanian women with ovarian cancer, and mostly occur in BRCA1/2. Given its clinical impact on disease prevention and precision therapy, universal testing should be routinely offered.

Phosphoinositide 3-kinase α (PI3Kα) is a propitious target for designing anticancer drugs. A series of new N’-(diphenylmethylene)benzenesulfonohydrazide was synthesized and characterized using FT-IR, NMR (1H and 13C), HRMS, and elemental analysis. Target compounds exhibited an antiproliferative effect against the human colon carcinoma (HCT-116) cell line. Our cheminformatics analysis indicated that the para-tailored derivatives [p-NO2 (3) and p-CF3 (7)] have better ionization potentials based on calculated Moran autocorrelations and ionization potentials. Subsequent in vitro cell proliferation assays validated our cheminformatics results by providing experimental evidence that both derivatives 3 and 7 exhibited improved antiproliferative activities against HCT-116. Hence, our results emphasized the importance of electron-withdrawing groups and hydrogen bond-acceptors in the rational design of small-molecule chemical ligands targeting PI3Kα. These results agreed with the induced-fit docking against PI3Kα, highlighting the role of p-substituted aromatic rings in guiding the ligand-PI3Kα complex formation, by targeting a hydrophobic pocket in the ligand-binding site and forming π-stacking interactions with a nearby tryptophan residue.

Background The chemical composition of Handal (Citrullus colocynthis L.) seed oil cultivated in Jordan deserts was characterized, and its bioactivity was evaluated. Methods The oil was extracted from the grinded seeds in 500 ml Soxhlet extractor for 24 hr using n‐hexane, and the recovered fatty acids were methylated with methanolic‐HCL. The fatty acid methyl esters (FAMEs) composition was analyzed using GC‐MS and GC‐FID. The anticancer activity associated with the oil was assessed against colon cancer cell lines (Caco‐2 and HCT‐116) and compared to its cytotoxicity on the human skin fibroblast. Multivariate analysis was used to determine relationship of the fatty acid composition with that of the anticancer activity. Results The results demonstrated that fatty acid composition of Citrullus colocynthis seed oil chiefly contains Linoleic acid, denoted as C18:2n6 (75%), followed by Palmitic acid C16:0 (8%), Stearic acid C18:0 (5%), and Oleic acid C18:1n9 (9%). It is demonstrated as an excellent source of essential fatty acids omega‐6 (e.g., Linoleic acid), whereas omega‐3 (e.g., α‐Linolenic acid) and hydroxy polyunsaturated fatty acids are found at small level. Interestingly, the oil exhibited reasonable anticancer effects against colorectal cancer cell lines with IC50 values varying between 4 and 7 mg/ml. The correlation test revealed a relationship between the fatty acid composition and the effectiveness on treatments. Conclusions Handal plant from Jordan appears to have very high level of Linoleic acid compared to other oils measured in different geographic locations and that there appears to be some anticancer activities associated with the fatty acid content of Handal seed oil.

Contemporary data on gender differences in outcomes after transcatheter aortic valve implantation (TAVI), after stratification by age, remain limited. We studied age-stratified (60 to 70, 71 to 80, and 81 to 90 years) inhospital outcomes by gender after TAVI from the National Inpatient Sample database between 2012 and 2018. We analyzed National Inpatient Sample data using the International Classification of Diseases, Clinical Modification, Ninth Revision, and Tenth Revision claims codes. Between the years 2012 and 2018, a total of 188,325 weighted hospitalizations for TAVI were included in the analysis. A total of 21,957 patients were included in the 60 to 70 age group (44% females), 60,770 (45% females) in the 71 to 80 age group, and 105,580 (50% females) in the 81 to 90 age groups, respectively. Propensity-matched inhospital mortality rates were significantly higher for females than males for the age group of 81 to 90 years (3.0% vs 2.1%, p0.01). Vascular complications and a need for blood transfusions remained significantly higher for females on propensity-matched analysis across all categories of ages. Conversely, acute kidney injury and the need for pacemaker implantation remained significantly higher for males across all age groups. In conclusion, we report that mortality is higher in female patients who underwent TAVI between the ages of 81 to 90. Moreover, the female gender was associated with higher vascular complications and bleeding requiring transfusions. Conversely, the male gender was associated with higher rates of pacemaker implantation and acute kidney injury.

A 48-year-old man presented with chest pain, dyspnoea, and cough with haemoptysis for one week. He had a history of unexplained hemopericardium requiring pericardiocentesis two months ago. TTE show...

Phosphoinositide 3-kinase α (PI3Kα) is a propitious target for designing anticancer drugs. A series of new N'-(diphenylmethylene)benzenesulfonohydrazide was synthesized and characterized using FT-IR, NMR (1H and 13C), HRMS, and elemental analysis. Target compounds exhibited an antiproliferative effect against the human colon carcinoma (HCT-116) cell line. Our cheminformatics analysis indicated that the para-tailored derivatives [p-NO2 (3) and p-CF3 (7)] have better ionization potentials based on calculated Moran autocorrelations and ionization potentials. Subsequent in vitro cell proliferation assays validated our cheminformatics results by providing experimental evidence that both derivatives 3 and 7 exhibited improved antiproliferative activities against HCT-116. Hence, our results emphasized the importance of electron-withdrawing groups and hydrogen bond-acceptors in the rational design of small-molecule chemical ligands targeting PI3Kα. These results agreed with the induced-fit docking against PI3Kα, highlighting the role of p-substituted aromatic rings in guiding the ligand-PI3Kα complex formation, by targeting a hydrophobic pocket in the ligand-binding site and forming π-stacking interactions with a nearby tryptophan residue.

e17593 Background: Ovarian cancer is one of the most common gynecological malignancies. Because of the absence of effective screening methods, ovarian cancer is usually diagnosed at late stages contributing to high mortality rates. Patients with BRCA1 and BRCA2 pathogenic germline variants (PGVs) harbor elevated risk of developing both ovarian and breast cancer. Identifying PGVs may help optimize management options and improve outcomes. The worldwide prevalence of gene mutations is variable. Multiple series have demonstrated differences in PGVs according to ethnicity and geographic area. Data about prevalence of the aforementioned PGVs among Arab patients with ovarian cancer is not well understood. Methods: Patients with epithelial ovarian, fallopian tube or primary peritoneal carcinomatosis were referred for 20 or 84-multi-gene panel testing (MGPT). All patients had their diagnosis, treatment and follow up at a single cancer center. Following detailed counselling, MGPT was performed at no-cost to all patients at two reference laboratories. Descriptive statistics were performed, groups outcome was determined by two-tailed Fisher’s exact test and unpaired t-test. The study was approved by the Institutional Review Board (IRB) at King Hussein Cancer Center and all patients signed informed consent. Results: During the study period, 152 patients, median age (range): 50 (18-79) years were tested. Two patients had fallopian tube cancer, while all others had epithelial ovarian cancer. The majority (n = 100, 65.8%) had high-grade serous carcinoma, and 106 patients (69.7%) had metastatic disease on presentation. In total, 38 (25.0%) had PGVs while 47 (30.9%) others had variants of uncertain significance (VUS). PGVs were mostly in BRCA1 (n = 21, 13.8%) and in BRCA2 (n = 12, 7.9%), while only 5 (3.3%) had PGVs in non- BRCA1/2 genes ( CHECK2, MUTYH, PMS2, RAD51D, and RB1) . Age (< 50 versus ≥50) at diagnosis, histological tumor subtype, and disease stage had no impact on pathogenic variant rates. However, PGVt rates were significantly higher (60.0%, p = 0.022) among patients with positive family history of ovarian cancer and 40.4% (p = 0.017) among patients with positive family history of breast cancer. The two patients with fallopian tube cancer were both positive for BRCA1 PGVs. Only one patient underwent prophylactic bilateral mastectomies. Conclusions: PGVs in patients with ovarian cancer are common among Arabs and mostly in BRCA1/2 and rates are significantly higher among patients with family history of ovarian or breast cancers.

1063 Background: The phase-3 MONALEESA-2,-3 and -7 randomized trials showed improved progression-free survival (PFS) and overall survival (OS) with the addition of cyclin D-cyclin-dependent kinase 4/6 (CDK4/6) inhibitor ribociclib to endocrine therapy in women with advanced-stage breast cancer. However, ribociclib induced acute renal injury is not recognized in these studies. In this report, we explore ribociclib-induced acute kidney injury (AKI) in breast cancer patients receiving ribociclib. Methods: We performed a retrospective chart review of all breast cancer patients who received ribociclib at our institution between April 2019 and September 2021. Patients and disease characteristics were collected, details of creatinine kinetics in relation to administration of ribociclib and other nephrotoxic drugs were obtained. Acute kidney injury grades (AKI-KDIGO classification) were captured. Results: 145 females, median age 60.0 years, all with advanced-stage breast cancer treated with aromatase inhibitors (AI) or fulvestrant plus ribociclib were reviewed. A total of 26 (17.9%) patients developed AKI; 3 were grade-I, 21 grade-II and 2 were grade-III. Rate of AKI was significantly higher (n = 15, 48.4%) among 31 patients on other concomitant nephrotoxic drugs, compared to 11 (9.6%) of 114 other patients, p = 0.001. Nephrotoxic drugs include non-steroidal anti-inflammatory (38%), metformin (30%), angiotensin-II receptor blockers (26%), and angiotensin-converting enzyme inhibitors (11%). Median time to develop AKI was 54 (range, 21-168) days, while the median time for creatinine recovery was 5 (range, 4-7) days after holding the drugs. Average creatinine increment for affected patients was 2.28 times the baseline level. Time to AKI was shorter, but not statistically significant, among patients on nephrotoxic drugs and recovery was faster after stopping these drugs (Table). Conclusions: Ribociclib-induced AKI is not uncommon and not adequately addressed. Though reversable in majority of patients, some patients may develop grade-III AKI or require treatment interruption. Nephrotoxic medications seem to significantly enhance ribociclib-associated renal injury. Withhold these medications with periodical assessment by nephrologist is strongly recommended in these patients. Larger studies are warranted to validate our findings. [Table: see text]

Background The chemical composition of Handal (Citrullus colocynthis L.) seed oil cultivated in Jordan deserts was characterized, and its bioactivity was evaluated. Methods The oil was extracted from the grinded seeds in 500 ml Soxhlet extractor for 24 hr using n‐hexane, and the recovered fatty acids were methylated with methanolic‐HCL. The fatty acid methyl esters (FAMEs) composition was analyzed using GC‐MS and GC‐FID. The anticancer activity associated with the oil was assessed against colon cancer cell lines (Caco‐2 and HCT‐116) and compared to its cytotoxicity on the human skin fibroblast. Multivariate analysis was used to determine relationship of the fatty acid composition with that of the anticancer activity. Results The results demonstrated that fatty acid composition of Citrullus colocynthis seed oil chiefly contains Linoleic acid, denoted as C18:2n6 (75%), followed by Palmitic acid C16:0 (8%), Stearic acid C18:0 (5%), and Oleic acid C18:1n9 (9%). It is demonstrated as an excellent source of essential fatty acids omega‐6 (e.g., Linoleic acid), whereas omega‐3 (e.g., α‐Linolenic acid) and hydroxy polyunsaturated fatty acids are found at small level. Interestingly, the oil exhibited reasonable anticancer effects against colorectal cancer cell lines with IC50 values varying between 4 and 7 mg/ml. The correlation test revealed a relationship between the fatty acid composition and the effectiveness on treatments. Conclusions Handal plant from Jordan appears to have very high level of Linoleic acid compared to other oils measured in different geographic locations and that there appears to be some anticancer activities associated with the fatty acid content of Handal seed oil., The chemical composition of Handal (Citrullus colocynthis L.) seed oil cultivated in Jordan deserts was characterized, and its bioactivity was evaluated.

Undifferentiated endometrial carcinoma (UEC) is a rare and poorly recognized entity, associated with a poor outcome. The clinical, pathologic, and immunohistochemical features of 17 cases diagnosed at our center are described. The median age was 60 yr. Postmenopausal bleeding was the most common presenting symptom (76.9%). Most patients presented with advanced stage (64.7%). Total hysterectomy with bilateral salpingo-oophorectomy was the commonly offered surgical treatment (80.0%). Nine (52.9%) patients received adjuvant treatment. The median overall survival was 11 mo. Pure UEC was seen in 8 cases (47.0%), while dedifferentiated carcinoma in 5 cases (29.4%). The epithelial component was part of carcinosarcoma or was mixed with serous carcinoma in 2 cases (11.8%) each. Positivity for one or more of the cytokeratin cocktails, mostly as strong focal staining, was evident in 16 cases (94.1%). PAX-8 was negative in 13 cases (86.7%). BRG-1/SMARCA4 was lost in 3 cases (20.0%). Eleven cases (64.7%) were MLH1/PMS2 deficient. Ten cases (66.7%) were positive for programmed death ligand 1, with positivity in 10%, 20%, and 100% of tumor cells detected in a single case each. Only 2 of 11 (18.2%) referral cases were correctly diagnosed as UEC. UEC is a rare tumor that is frequently misdiagnosed. A panel of immunostains is necessary to make the correct diagnosis. The range of positivity for programmed death ligand 1 testing suggests that immunotherapy might be considered in the adjuvant setting, especially with the poor response of this tumor to traditional therapies.

A new series of imidazole-5-carboxamide derivatives were prepared and tested for their anti-hyperlipidemic activity in Triton-WR-1339-induced hyperlipidemic Wistar rats. The purpose of this research was to improve benzophenone carboxamides water solubility maintaining at the same time the antihyperlipidemic activity. Compounds 4, 6, 10, and 11 were synthesized through a coupling reaction between imidazoles-5-carbonyl chloride and amino benzophenones. The tested animals (n=48) were divided into six groups: the first group (hyperlipidemic control group; HCG) received an intraperitoneal injection (i.p.) of (300 mg/kg) Triton WR-1339. The second group received i.p. injection of Triton WR-1339 followed by an intra-gastric administration of bezafibrate (100 mg/kg) (bezafibrate; BF). The third, fourth, fifth, and sixth groups received i.p. injection of Triton WR-1339 followed by an intra-gastric administration of (30 mg/kg) of compounds 4, 6, 10, and 11, respectively. At a dose of 30 mg/kg body weight compounds 4, 6, 10, and 11 significantly (p

Background: Antibiotics are important drugs used against bacterial infections. Unfortunately, overusing them resulted in the development of resistant bacteria. There are limited data concerning antibiotic use so we worked on this study to provide more updated data. Objective: The aim of this study was to assess public knowledge, attitude and practice regarding antibiotics use and related factors in Riyadh – KSA. Method: It was a cross-sectional online and manual survey involving 474 respondents and was conducted in Riyadh, KSA in February 2016. The collected data were analyzed using SPSS version 20. Results: Most of the respondents (86.5%) had used antibiotics for others (friends and family). Only 7% of respondents had good knowledge and about 50% of them had negative attitudes. Respondents' educational level was a predictor of negative attitude as those with a low level of education (below secondary) 66.7% were more likely to show negative attitude compared to those with high educational level (university and above; 40%). Poor level of knowledge was a predictor of negative attitude; as 65% of respondents with poor knowledge showed a negative attitude compared to only 24.2%; those with a good level of knowledge. Conclusion: This study concluded that females and married participants showed better practice toward antibiotics use. Higher education level was strongly associated with better knowledge, attitude, and practice and was not associated with an increased risk of self-medication. Respondents with high income and those with better knowledge exhibited better practice.

Background: Oncogenic potential of phosphatidylinositol 3-kinase (PI3Kα) has been highlighted as a therapeutic target for anticancer drug design. Objective: Target compounds were designed to address the effect of different substitution patterns at the N atom of the carboxamide moiety on the bioactivity of this series. Methods: Synthesis of the targeted compounds, crystallography, biological evaluation tests against human colon carcinoma (HCT-116), and Glide docking studies. Results: A new series of N-substituted- 4-hydroxy-2-quinolone-3-carboxamides was prepared and characterized by means of FT-IR, 1H and 13C NMR, and elemental analysis. In addition, the identity of the core nucleus 5 was successfully characterized with the aid of X-ray crystallography. Biological activity of prepared compounds was investigated in vitro against human colon carcinoma (HCT-116) cell line. Results revealed that these compounds inhibit cell proliferation and induce apoptosis through an increase in caspase-3 activity and a decrease in DNA cellular content. Compounds 7, 14, and 17 which have H-bond acceptor moiety on p-position displayed promising PI3Kα inhibitory activity. On the other hand, derivatives tailored with bulky and hydrophobic motifs (16 and 18) on o- and m-positions exhibited moderate activity. Molecular docking studies against PI3Kα and caspase-3 showed an agreement between the predicted binding affinity (ΔGobsd) and IC50 values of the derivatives for the caspase-3 model. Furthermore, Glide docking studies against PI3Kα demonstrated that the newly synthesized compounds accommodate PI3Kα kinase catalytic domain and form H-bonding with key binding residues. Conclusion: The series exhibited a potential PI3Kα inhibitory activity in HCT-116 cell line.

Hyperlipidemia is known as an elevation of plasma lipid components. It contributes significantly to atherosclerosis which is one of the most important causative factors in cardiovascular diseases. Agents that cause a dramatic decrease in serum lipid levels are of great value in the treatment of cardiovascular diseases. For this purpose, a new series of benzimidazole propyl carboxamide benzophenone derivatives have been synthesized (7, 8, and 9). These compounds were tested in vivo to evaluate their potential hypolipidemic activity using Triton WR-1339 induced hyperlipidemic rats. All the synthesized compounds have proved to be highly biologically active, with compound 9 being the most active derivative.

A new series of thiosemicarbazone-based indole derivatives 12–15 has been prepared by condensation reaction of indole-2-carboxamide derivatives 8–11 with thiosemicarbazide. The former compounds underwent intracyclization in the presence of chloroacetic acid and sodium acetate to afford a set of new 3-(indol-2-yl)bicyclotetrazatridecahexaens 16–19. These newly synthesized compounds have been characterized by means of FTIR, 1H NMR, 13C NMR, and HRMS and by elemental analyses. Cytotoxic activities of the prepared compounds along with LY294002 were evaluated in vitro against normal human skin fibroblast, human colon carcinoma (HCT116), and leukemia (K562) cell lines; results revealed that the series inhibits only HCT116 cell line. In addition, results showed that compound 18 exerts moderate potency in HCT116 with an IC50 value of 54 μmol/L and significantly induces apoptosis.

Bladder cancer is the most common cancer of the urinary tract with an estimate of 401,000 new cases diagnosed annually worldwide. In Jordan, bladder cancer accounts for 4.3% of all newly diagnosed cancer cases. Several studies have linked p53 molecular changes to tumor initiation, invasion, metastasis, and chemoresistance. In the present study, we investigated a cohort of 121 bladder cancer patients with various grades and stages of the tumor for molecular changes in p53. Overexpression of p53 was shown in 22%, 46%, 71% and 25% pTa, pT1, pT2 and pT4 cases, respectively. Additionally, p53 was overexpressed in 19%, 38% and 74% of G1, G2 and G3 cases of bladder cancer, respectively. p53 expression is not significantly associated with the stage or grade of the disease. Mutational analysis of exons 4–8 of p53 identified the following previously reported point mutations R72P (58%), P67T (9%), A159P (0.7%), D185N (28%), G199 V (0.7%), G199E (0.7%), D208N (0.7%), R283P (1.4%). Furthermore, we were able to identify two new deletion mutations located in the DNA-binding domain in two patients. The first mutation was a result of one nucleotide deletion in exon 5 causing a frameshift at codon 115 resulting in a truncated 168 amino acids long p53 protein and the second is a result of a whole codon deletion in exon 6 resulting in a p53 protein missing a valine residue at codon 218. P53 mutations were found to be significantly associated with late stage (pT2-pT4) muscle-invasive bladder tumors. Survival analysis indicates significant differences of overall survival between the patients with the p53 overexpression and those with negative p53 staining ( p = 0.0041). Additionally, were able to observe a significant difference of overall survival between p53 mutants and p53 wild-type ( p = 0.0062). The present work points to the variable spectrum of TP53 mutations and p53 expression profile in Jordanian patients with bladder cancer and reflects the importance of p53 alterations in predicting poor prognosis of bladder cancer patients.

Hyperlipidemia is a known cause of coronary vascular diseases, which is a major cause of death in many parts of the world. Targeting several pathways that lead to increase in lipid profiles is of great potential to control diseases. 1H-indole-2-carboxamide derivatives were tested for their hypolipidemic activity at the molecular level in comparison with bezafibrate. The gene expression profiles of lipoprotein signaling and cholesterol metabolism and fatty acid metabolism PCR arrays were determined in rats with acute hyperlipidemia induced by Triton WR1339. Lipid profiles of serum from treated rats showed significant hypolipidemic effect by the compounds. Several genes of potential interest were reported to be overexpressed by Triton WR1339 including Apoc3, Apob, Hmgcs2, Apoa1, Apoe, Apof, acsl1, and Decr1. Most of the overexpressed genes were downregulated by N-(3-Benzoylphenyl)-1H-Indole-2-Carboxamide with significant decreases in Apoc3, Apob, Acaa2, Acsl1, and Slc247a5 gene expression levels. N-(4-Benzoylphenyl)-1H-Indole-2-Carboxamide and bezafibrate did not significantly affect the gene expression levels which were increased with acute hyperlipidemia induced by Triton WR1339. In conclusion, gene expression profiling identified the possible mechanism in which Triton WR1339 induces its acute hyperlipidemic effect which was reversed by the use of N-(3-Benzoylphenyl)-1H-Indole-2-Carboxamide.

Structure-based drug design and molecular modeling were employed to identify a new series of indole-2-carboxamides as potential anticancer agents. These compounds were synthesized and characterized with the aid of several spectroscopic techniques, such as FT-IR, NMR, and mass spectrometry as well as by elemental analysis. Molecular docking studies confirmed that the newly synthesized compounds accommodate PI3Kα and EGFR kinase catalytic sites and form H-bonding with the key binding residues. The antitumor activity of these new compounds against an array of cancer cell lines (human colon carcinoma (HCT116), leukemia (K562), and breast cancer (MDA231) was evaluated. Results revealed that these compounds were selective against the kinase domain, and none of them showed any inhibitory activity against K562. In addition, results showed that compound 13 exhibited high potency in HCT116 and MDA231 with IC50 values of 19 and 15μM, respectively. Our findings recommend that further optimization of this series would be beneficial for colon and breast cancer treatment.