Synthesis and anticancer activity of (E)-2-benzothiazole hydrazones

• Published in: European journal of medicinal chemistry Vol. 86; pp. 12 - 16
• Main Authors: Lindgren, Eric B., de Brito, Monique A., Vasconcelos, Thatyana R.A., de Moraes, Manuel O., Montenegro, Raquel C., Yoneda, Julliane D., Leal, Kátia Z.
• Format: Journal Article
• Language: English
• Published: ISSY-LES-MOULINEAUX Elsevier Masson SAS 30.10.2014; Elsevier
• Subjects: (E)-2-benzothiazoles; Anticancer; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Benzothiazoles - chemical synthesis; Benzothiazoles - chemistry; Benzothiazoles - pharmacology; Cell Line, Tumor; Cell Proliferation - drug effects; Chemistry, Medicinal; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; HL-60 Cells; Humans; Hydrazines - chemical synthesis; Hydrazines - chemistry; Hydrazines - pharmacology; Hydrazones; Life Sciences & Biomedicine; Lipinski's rule of five; Molecular Structure; Pharmacology & Pharmacy; Science & Technology; Structure-Activity Relationship; (E)-2-benzothiazoles; Hydrazones; Lipinski's rule of five; Anticancer; ANTIMYCOBACTERIAL ACTIVITY; ANTITUMOR EVALUATION; ORAL BIOAVAILABILITY; DOXORUBICIN; DERIVATIVES
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2014.08.039

Benzothiazole hydrazones have been synthesized and evaluated for their in vitro antiproliferative activity against three human cancer cell lines: HL-60 (leukemia), MDAMB-435 (breast) and HCT-8 (colon). The good cytotoxicity for the three cancer cell lines and theoretical profile of compounds 3o and 3p pointed them as promising lead molecules for anticancer drug design. [Display omitted] •Benzothiazole hydrazones were synthesized.•Antiproliferative activity of these compounds was evaluated.•Compounds 3n and 3o showed significant cytotoxicity against leukemia (HL-60).•Compounds 3o and 3p exhibited cytotoxicity against three cancer cell lines.•Benzothiazole hydrazones bear hydroxyl groups may have a good oral biodisponibility.