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Pyrrole is a biologically active scaffold, which itself possess noticeable anticancer activity against several types of cancer specially leukemia, lymphoma, and myelofibrosis. SAHA and its synthetic analogs has demonstrated potent antitumor activity against numerous human cancer lines and different classes of HDACs. The HDAC inhibitor possessing pyrrole as linker moiety has been developed for anticancer property. The objective of present studies was to incorporate pyrrole as connecting unit in hydroxamic acid based HDAC inhibitors for their anticancer evaluation and molecular docking studies. A series of novel 4-substituted methyl 6-(3-acetyl-2-methyl-1H-pyrrol-1-yl)hexanoate [3(a-z)] and 4-substituted 6-(3-acetyl-2-methyl-1H-pyrrol-1-yl)-N-hydroxyhexanamide [4(a-z)] were synthesized. These analogs were evaluated for their anticancer activity using in-vitro method against leukemia (K-562), lung (A-549), breast (MCF-7), and cervical (HeLa) human cancer cell lines using Sulforhodamine B (SRB) assay method, HDAC1 and HDAC6 inhibitory assay and binding mode analysis using molecular docking studies. The in-vitro studies of 3(a-z) indicated that substitution with electron donating groups produces active or moderately active compounds. Interestingly, p-nitro-substituted molecule produced a most active derivative in the series. The in-vitro anticancer study of 4(a-z) indicated that the unsubstituted phenyl derivative, 6-(3-acetyl-2-methyl-4-phenyl-1H-pyrrol-1-yl)-N-hydroxy-hexanamide (4a) have moderate antitumor activity against K-562 human leukemia cell line. Substitution at 4-phenyl ring with weak and moderate electron withdrawing groups, such as fluoro, chloro, and bromo potentiated the cytotoxic activity. The 4(a-z)] were docked against different HDAC proteins to determine the exact binding mode and orientation. These synthetic analogs have similar binding mode as SAHA on the active pocket. The pyrrole based novel SAHA analogs 3(a-z) and 4(a-z) displayed promising anticancer activity. These studies can be further employed for the design and development of novel SAHA analogs with promising anticancer activity.

In the pasture of oncology, anticancer agents having advanced modes of action are of great interest because of increasing chronicity of resistance against anticancer drugs. Heterocyclic scaffolds like benzothiazoles are reported to display an extensive range of pharmacological activities including anticancer, anti-tubercular, antiviral, fungicidal, etc. and are indispensable tools for the researchers involved in vistas of chemistry for proposing of novel anticancer drugs. Benzothiazole scaffold is a bicyclic organic compound having benzene ring fused with heterocyclic nucleus (thiazole) containing sulphur and nitrogen atoms that possess a wide range of different pharmacological activities and are still of grand and logical concern nowadays. Interesting pharmacological activities are exhibited by benzothiazoles and they were developed as successful inhibitors of a variety of biological targets such as tubulin polymerase inhibitor, DNA topoisomerase-inhibitor, an Abl kinase inhibitor, HDAC inhibitor, Aurora-B kinase inhibitor. This review highlights the latest research on the structure-activity relationship of benzothiazole scaffold against different biological targets for their anticancer activity. This survey additionally addresses the recent patents granted and novel advancement made through the application of nanocarriers in recent decades with thorough talk of benzothiazoles as conceivable anticancer mediators which may be helpful for the emerging scientific pursuits.

Cancer is a very risky life-threatening disease having most formidable afflictions in the world. Several anticancer agents are commercially accessible, however, the emergence of acquired drug resistance along with extreme adverse effects of these clinically used anticancer medications are major barriers to the effective chemotherapy. Thus, it is recommended to rationally design the newer drugs with few side effects. Fluoroquinolone derivatives are of pivotal interest for researchers due to their admirable pharmacological and pharmacokinetic profiles. They exhibit several favourable characteristics including, higher bioavailability, excellent tissue penetration and relatively low prevalence of adverse and toxic effects. Due to their potential interventions in carcinogenesis and mutagenesis, the focus of the area of research is nowadays shifting towards anticancer aspects of these compounds. This review shows the recent advancements in the development of novel fluoroquinolones as potential anticancer and cytotoxic agents and structure-activity relationships along with the possible modes of action for further development and recent patents filed/granted related to anticancer activity from the last few years have also been tabulated. Also, this review is an attempt to focus on the various upcoming aspects of fluoroquinolones and provides a newer outlook on the possible roles of fluoroquinolones in the treatment of cancer. Scientific information identified in this paper is expected to be useful for aspiring researchers working on the anticancer activity of fluoroquinolones.

Two novel series of N4-(5-(2/3/4-substituted-phenyl)-1,3,4-oxadiazol-2-yl)-N1-(2-methyl-5-(prop-1-en-2-yl)cyclohex-2-enylidene)semicarbazide and N4-(5-(2/3/4-substituted-phenyl)-1,3,4-oxadiazol-2-yl)-N1-(3,7-dimethylocta-3,6-dienylidene)-semicarbazide were synthesized to meet structural prerequisite indispensable for anticonvulsant activity. The anticonvulsant activities of the compounds were investigated using maximal electroshock seizure (MES), subcutaneous pentylenetrtrazole (scPTZ) and subcutaneous strychnine (scSTY) models. The rotorod test was conducted to evaluate neurotoxicity. Some of the selected active compounds were subjected to GABA assay to confirm their mode of action. The outcome of the present investigations proved that the four binding sites pharmacophore model is vital for anticonvulsant activity. The efforts were also made to establish structure–activity relationships among test compounds.

Histone deacetylase inhibitors have been actively explored as a new generation of chemotherapeutics for cancers, generally known as epigenetic therapeutics. Two novel series of N-(2-amino-phenyl)-4-{[(2/3/4-substituted-phenylcarbamoyl)-methyl]-amino}-butyramide and N-(2-amino-phenyl)-4-{[(2/3/4-substituted-phenylcarbamoyl)-methyl]-amino}benzamide were designed and synthesized as novel histone deacetylase inhibitors. The anticancer potential of the compounds were determined in-vitro using MTT assay against HCT-116 and U251 (glioma) cell lines and histone deacetylase inhibitory assay. The synthesized compounds were investigated for anti-tumor activity against Ehrlich ascites carcinoma (EAC) cells in Swiss albino mice. The efforts were also made to ascertain structure-activity relationships among test compounds. The results of the present studying represents appraisal of γ-aminobutyric acid (GABA) and para-aminobenzoic acid (PABA) as linker moiety for development of newer benzamide based histone deacetylase inhibitor.

In pursuit for better antiepileptic drug and the importance of semicarbazones and 2,5-disubstituted 1,3,4-thiadiazoles as anticonvulsant pharmacophore, a series of novel N -({5-[(6-methyl-1-benzofuran-3-yl)methyl]-1,3,4-thiadiazol-2-yl}carbamothioyl)-2/3/4-substitutedbenzamide were designed, synthesized and evaluated for their anticonvulsant activity. The findings of the present studies confirmed that the pharmacophore model with four binding sites is crucial for anticonvulsant activity. Structure–activity relationships among synthesized compounds were also established.