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The present review supply an overview of the chemistry of (aryl/hetaryl)thiopyran-4-one derivatives via a systematic and comprehensive survey of thesynthetic methods, the chemical reactivity and bi...

The following review article provides an overview of DHA chemistry, with specific confirmation based on major historical developments and progress mainly made over the last two decenniums. It is our hope this review serves as a valuable treasure to those interested in the 3-acetyl-4-hydroxy-6-methyl-2H-pyran-2-one (DHA) chemistry, and helps impact future advancements.

This review supply an inclusive survey of the recent progress in the chemistry of 4,6‐dimethyl-3-amino-3H-pyrazolo[3,4-b]pyridine concerning the synthesis and reactions and biological activity over...

This review summarizes the most common synthetic routes as applied to the preparation of many modern pharmaceutical compounds categorized as 2-amino-3-cyano-quinoxaline 1, 4-dioxide and its derivat...

The new thiopyrano[2,3- b ]pyridines 4 – 9 could be synthesized from the nicotinonitrile derivative 1 . The cytotoxicity activity of the selected compounds 5 , 6 and 8 was tested against MCF-7 and HCT -116 cell lines. The compound 5 ( TP 5 ) exhibited significant inhibitory activity and displayed the most potent activity, more than 6 and 8 . The compound 5 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent. In the light of this result, the labeled 125 I-compound 5 ( 125 I -TP 5 ) was prepared and its cytotoxicity against ascites tumor in mice has been evaluated. The results show that compound 5 ( TP 5 ) may be potentially used as a radiopharmaceutical for tumor diagnosis when labeled with 125 I.

Thesis Abstract Triazines represent a promising scaffold for cancer treatment due to their similarity to the biologically active purine and pyrimidine systems. Besides, triazines and annulated compounds exist in the skeleton of numerous natural and synthetic chemotherapeutic agents such as Azanucleosides (6-azacytosine and 6-azauracil). Also, triazine derivatives proved to display antiviral, anti-inflammatory, antimicrobial and antifungal activities. Moreover, it was found that triazine derivatives display significant wide spectrum anticancer activities against lymphoblastic lung adenocarcinoma A549, leukemia CEM and myeloid leukemia K562 cancer cell lines. In this regard, newly series of triazine-based thiadiazol, thiadiazine, thiadiazepine, pyrazole tetrazepino[b]indol-one, triazolotriazine, tetrazolotriazine, triazinotetrazine, and triazinotetrazepinoindole moieties were synthesized, spectrally discussed and mechanistically discussed. On the other hand, the synthesized compounds were evaluated against different types of biological bioassays (Antitumor, Antioxidant and Antimicrobial). Also, compounds 33c and 37 were evaluated against three human cancer cell lines (HepG‐2, HCT‐116, and MCF‐7) for their in-vitro anticancer activities. The results declared that all compounds had a potent anticancer activity with IC50 values ranging between 10.8 and 23.4 μM.

Thesis Abstract: Coumarin compounds are one of the most active classes of heterocyclic compounds. They play active roles in medicine due to their biological activity. These compounds are found in many natural products. Hydroxylochocarpin (a), lonchocarpin (b) and lonchocarpene (c) are used as anticancer reagents. Moracin D (d) used as an antifungal while cromakalim (e) produces anti-hypertensive effects and SD-8381(f) produces anti-inflammatory effects as a new cyclooxygenase inhibitor. Catechin (g) and epigallocatechin gallate [EGCG] (h) both represent antiallergic and anticancer effects, while KRH-102140 (i) is identified as a5-lipoxygenase (5-LO) inhibitor. Seseline (j) and xanthylein (k) exhibit anticancer activities. Rotenone (l) used as an anti-anaphylactic agent for treating asthma. Also dronabinol [∆9-THC] (m) and other cannabinoids used for treating symptoms of cancer. Suksdorfin (n) inhibits the human immunodeficiency virus (HIV) while daleformis (o) inhibits the endothelin-converting enzyme. The aim of the present work is to design and synthesize fused bicyclic and polycyclic ring systems via enamino derivatives incorporating benzopyrone moiety (coumarin structure).

Thesis Abstract: 2-acetylphenothiazine plays an important role in organic chemistry. The behavior of 2-acetylphenothiazine towards various reagents was carried out. Thus, the aim of the present work is to design and synthesize some of heterocyclic nuclei through the reaction of phenothiazine derivatives as scaffold moiety with different reagents. α,β-Unsaturated ketones containing phenothiazine moiety 4, 5, 7 were synthesized by condensation of 2-acetylphenothiazine with different aryl aldehydes 2, 3, and (DMFDMA). Pyrazole skeletons were also synthesized by 1,3-dipolar cycloaddition reactions of α,β-unsaturated ketones with different nucleophilic reagents. Formylpyrazole derivative 36 was synthesized through the Vilsmeier-Haack reaction of phenylhydrazone 35b. Azines derivatives of phenothiazines were synthetically constructed from one-pot multicomponent reactions of 1-(4a, 10a-dihydro-10H-phenothiazine-2-yl) ethan-1-one with various reagents. Newly synthesized compounds were screened as antioxidant agents. The sequence of these reactions that adopted for the synthesis of the designed compounds in this thesis is summarized into two sections. Furthermore, studying of the biological activity of the newly synthesized compounds as antioxidants properties were performed.

Heterocyclic compounds containing nitrogen, oxygen and sulfur atoms possess various interesting biological activities. Among these compounds, 1,3-oxathiolan-5-one and its diverse derivatives which are literature documented ones of the most potent core structures in drug design and pharmaceutical industry. This thesis describes the utility of 1,3-oxathiolan-5-one in the synthesis of pyridinonethiol and their annulated systems through multicomponent reaction of 2-methyl-2-phenyl-1,3-oxathiolan-5-one (1), aniline and α,β-unsaturated carbonyl compounds. On the other hand, different bioactive heterocyclic systems such as thiophene, furo-oxathiolone, mercapto-diphenylcyclopenta-2,4-dien-one, triazole and thiadiazine have been efficiently synthesized via tandem reactions of 1,3-oxathiolan-5-one 1 with different nucleophilic reagents. The structures of newly synthesized compounds were confirmed by spectral data, elemental analyses and mechanically discussed. Also, in vitro antioxidant and antitumor activities of these compounds were evaluated. In addition, the synthesized compounds were screened against hepatic cancer cell line HepG-2, as the optimistic results exhibited that compounds 29, 33 and 34 have excellent antioxidant and anti HepG-2 activities.