Synthesis and Evaluation of Some Novel Benzothiazole Derivatives as Potential Anticancer and Antimicrobial Agents

Abstract

Intensive efforts are underway worldwide to develop anticancer and antimicrobial agents. Therefore, a novel series of pyri-do[2,1-b]benzo[d]thiazole and 2-(benzo [d]thiazol-2-ylamino)pyrimidine derivatives was synthesized. The synthesized compounds were evaluated for their anti-cancer activity. Among the tested compounds, compounds 3a, 3b, and 7 exhibited more cytotoxic action than the control drug doxorubicin (CAS 23214-92-8; IC₅₀: 52 µg/ml). Compound 7 was the most potent cytotoxic, with an IC₅₀ of 42.55 µg/ ml, while compounds 3a and 3b induced high cytotoxic action with IC₅₀ values of 50.15 µg/ml and 50.45 µg/ml, respectively.

Moreover, the synthesized compounds were screened for their antibacterial and antifungal activities. Compound 6 exhibited moderate antifungal activity against C. albicans with a minimum inhibitory concentration of 125 µg/ml.

Key words

Anticancer agents - 2-(Benzo[d]thiazol-2-ylamino)pyrimidines, anti-cancer activity - antimicrobial activity - Ehrlich ascites carcinoma - Pyrido[2,1-b]benzo[d]thiazoles, anticancer activity - antimicrobial activity