Abstract
A series of novel betulin-28-hydrazone derivatives (7a-7o) were synthesized. All compounds were evaluated for their in vitro cytotoxicities in four human carcinoma cells (HepG2, MCF-7, HCT-116 and A549). Among them, compound 7l displayed the most potent cytotoxicity with an IC50 (concentration of the tested compound that inhibits 50% of cell growth) value of 7.37 ± 0.38 μM against MCF-7 cells. The preliminary cellular mechanism studies indicated that compound 7l could induce MCF-7 cells apoptosis. The above findings indicated that compound 7l may be used as a lead compound for antitumor agents with improved efficacy.
Highlights
IntroductionCancer has become the second leading cause of death worldwide.[1]. The most effective of therapies used in cancer treatment continue to be traditional cytotoxic agents.[2]
Nowadays, cancer has become the second leading cause of death worldwide.[1]
The general procedure for the synthesis of betulin derivatives is shown in Scheme 1
Summary
Cancer has become the second leading cause of death worldwide.[1]. The most effective of therapies used in cancer treatment continue to be traditional cytotoxic agents.[2]. The solution was evaporated and redissolved with CH2Cl2 (100 mL), washed with brine twice and dried over anhydrous Na2SO4. Betulin-28-(benzylidene)hydrazone (7a) White solid; 73%; 1H NMR (600 MHz, CDCl3) d 8.50. Betulin-28-(4-chloro-benzylidene)hydrazone (7c) Pale yellow solid; 75%; 1H NMR (600 MHz, CDCl3). Betulin-28-(4-bromo-benzylidene)hydrazone (7d) Pale yellow solid; 72%; 1H NMR (600 MHz, CDCl3). Betulin-28-(4-nitro-benzylidene)hydrazone (7g) Pale yellow solid; 79%; 1H NMR (600 MHz, CDCl3). Betulin-28-(3-trifluoromethyl-benzylidene)hydrazone (7h) Pale yellow solid; 82%; 1H NMR (600 MHz, CDCl3). Betulin-28-(furan-2-ylmethylene)hydrazone (7o) Pale yellow solid; 72%; 1H NMR (600 MHz, CDCl3). The cells were treated with compounds at gradient concentrations from 1 to 60 μM for 48 h and 10 μL MTT (Sigma Chemical Co., Ltd., Milwaukee, USA) solution (5 mg mL–1 in phosphate buffered saline (PBS)) were added for 2 h. The cells apoptosis analysis was examined by flow cytometry and system software (BD Biosciences, San Jose, CA, USA).[40]
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