Design, synthesis and biological evaluation of 1,2,3-Triazole ring incorporated (1,3,4-thiadiazol-2-yl)pyrimidin-5-yl)-3-(4-nitrophenyl)-1,2,4-thiadiazole derivatives as anticancer agents

IF 2.4 Q2 Chemistry

Chemical Data Collections Pub Date : 2026-03-01 Epub Date: 2026-02-16 DOI:10.1016/j.cdc.2026.101232

Batta Kondala Rao , Reddymasu Sreenivasulu , Somaiah Nalla , Kiranmayi Peddi

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引用次数: 0

Abstract

A new library of 1,2,3-triazole ring incorporated (1,3,4-thiadiazol-2-yl)pyrimidin-5-yl)-3-(4-nitrophenyl)-1,2,4-thiadiazole (11a-j) have been designed and synthesized. Further, the anticancer activity of the newly synthesized compounds 11a-j is screened against a panel of four type’s human cancer cell lines such as PC3 (human prostate cancer), A549 (human lung cancer), MCF-7 (human breast cancer) and A2780 (human ovarian cancer) by employing the MTT method. The achieved outcomes were incorporated in Table 1, and were compared with etoposide as positive control. Almost all the tested derivatives displayed noticeable activity as etoposide. Among all, six compounds 11a, 11b, 11g, 11h, 11i and 11j displayed remarkable activity than positive control. Mainly, one compound 11a showed superior activity against PC3, A549, MCF-7 and A280 cell lines with IC₅₀ values of 0.04±0.0087 µM; 0.06±0.0069 µM; 0.02±0.0054 µM & 0.22±0.0048 µM respectively.

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1,2,3-三唑环含（1,3,4-噻二唑-2-基）嘧啶-5-基)-3-（4-硝基苯）-1,2,4-噻二唑抗癌衍生物的设计、合成及生物学评价

设计并合成了含有（1,3,4-噻二唑-2-基）嘧啶-5-基)-3-（4-硝基苯基）-1,2,4-噻二唑（11a-j）的1,2,3-三唑环文库。此外，采用MTT方法对新合成的化合物11a-j对PC3（人前列腺癌）、A549（人肺癌）、MCF-7（人乳腺癌）和A2780（人卵巢癌）等四种类型的人癌细胞系进行了抗癌活性筛选。获得的结果纳入表1，并与依托泊苷作为阳性对照进行比较。几乎所有被测衍生物都显示出明显的依托泊苷活性。其中，化合物11a、11b、11g、11h、11i和11j的活性显著高于阳性对照。其中化合物11a对PC3、A549、MCF-7和A280细胞系的IC50值为0.04±0.0087µM；0.06±0.0069µM;分别为0.02±0.0054µM和0.22±0.0048µM。

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来源期刊

Chemical Data Collections Chemistry-Chemistry (all)

CiteScore

6.10

自引率

0.00%

发文量

169

审稿时长

24 days

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