4‐Chlorothiazole‐5‐carbaldehydes as Potent Precursors for Synthesis of Some New Pendant N‐heterocyces Endowed with Anti‐Tumor Activity

Abstract

In our approach to synthesize bioactive molecules, a series of novel N‐heterocycles were synthesized and evaluated for their in vitro antitumor activity against a panel of three human cancer cell lines, namely, human breast cancer cell line (MCF‐7), human cervical cancer cell line (HeLa), and human prostate cancer PC‐3. The majority of the tested compounds exhibited significant cytotoxic activity toward the tested tumor cell lines. Analogues 33, 34, 31, 38, 21, 23, 22, and 20 exhibited considerable cytotoxic activities comparable with standard drug 5‐fuorouracil. Compound 33 displayed superior cytotoxicity with IC50 value of 4.12 ± 1.21 μg/mL against HeLa tumor cell line.

Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

“…Of this class, 1,2,4-triazines [7][8][9][10][11][12][13] and 1,2,4-triazoles [14][15][16][17][18][19][20][21], as well as pyrimidines [22,23], have been introduced in a renewed generation of medication. Due to our interest in these azines, their ligation, and modification, we revisited and continued upon our previous research projects [24][25][26][27][28][29][30] with this study. We describe the annulation and in vitro preliminary antimicrobial impact of new 8-phenyl-6-(thiophen-2-yl)-6,7-dihydro-2H-pyrimido[2,1-c] [1,2,4]triazine-3,4-dione tripod-based congeners.…”

Design, Synthesis and Pharmacological Evaluation of Novel Annelated Pyrimido[2,1-<em>c</em>][1,2,4]Triazolo[3,4-<em>f</em>][1,2,4]Triazines as Antimicrobial Agents

“…Our starting point is to prepare 8-phenyl-6-(thiophen-2-yl)-6,7-dihydro-2H-pyrimido [2,1c][1, 2,4] triazine-3,4-dione (2), as a versatile precursor for annulation the target novel N-heterocyclic systems, to evolve probes of admirable therapeutic potentials. So, treatment of the hydrazonyl analogue 1 [35,36], with oxalyl chloride in refluxing DMF containing Et3N as catalyst, afforded the 1,2-dioxo-triazine analogue 2. The cyclic 1,2-bioxygen analogues are well known to be reactive, and were utilized as potential precursors for building various heterocyclic systems, that can possess awaited biological activity.…”

“…On the other hand, considering the antifungal activity, the trend altered and compound 15d was the most potent antifungal analogy, having (MeO) group as an electron releasing substituent at para position in its phenyl ring. 2-Hydrazinyl-6-phenyl-4-(thiophen-2-yl)-4,5-dihydropyrimidine (1) was synthesized according to the reported work [35,36]. Physical, analytical and spectral data are given in tables 1 and 2.…”

“…Physical, analytical and spectral data are given in tables 1 and 2. They were synthesized, according to our reported work [35,36]. mmol) in dioxane (20 mL) was added dropwise.…”

An Efficient Synthetic Approach Towards Benzo[b]pyrano[2,3-e][1,4]diazepines, and Their Cytotoxic Activity

“…Due to our admiration with the synthesis, modification, and studying the biological activities of benzodiazepines, herein, we freshened our sustained efforts [21][22][23][24][25][26][27], through the synthesis and utility of 5-methyl-4-(methylthio)- 2-oxo-2,11-dihydrobenzo[b]pyrano [2,3-e] [1,4]diazepine-3-carbonitrile (5) as a reactive precursor, for the annulation of benzopyranodiazepines of potential biological activity.…”