Synthesis of Novel Benzothiazolo[3,2‐ a ]pyridimidin‐4‐ones with Potential Cytotoxic and Pro‐Apoptotic Potential

Behzad Jafari, Faisal M. Rashid, Sayfidin Shahobidinovich Safarov, Meirambek Ospanov, Nazym S. Yelibayeva, Zharylkasyn A. Abilov, Mirgul Zh. Turmukhanova, Sergey Kalugin, Peter Ehlers, Muhammad Ihtisham Umar

3 more authors

Sumera Zaib, Jamshed Iqbal, Peter Langer

2018

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DOI 10.1002/slct.201802426

Data confidence 70 medium

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Abstract

Abstract The combination of cyclocondensation with palladium catalysed cross‐coupling reactions, afforded a variety of 8 ‐ functionalized benzothiazolo[3,2 ‐ a ]pyridimidin ‐ 4‐ones in good to excellent yields. The anti‐proliferative potential of the synthetic compounds was evaluated in human cervical adenocarcinoma cells (HeLa) and hamster normal fibroblasts (BHK‐21). Three of the test derivatives exhibited the strongest cytotoxicity in HeLa cells with the median inhibitory concentration (IC 50 ) of 0.93, 1.55 and 1.84 μM, respectively. Moreover, their anti‐proliferative effect was three times less strong in normal fibroblasts, asserting their possible anti‐cancer potential.