2008
DOI: 10.3892/ijmm.21.4.477
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Synthesis and antitumor activity of aromatic camptothecin esters

Abstract: Abstract. Twenty-eight new aromatic esters of camptothecins 2-29 were prepared in yields of 5 to 96% by straight acylation of camptothecin (1a) and 9-nitrocamptothecin (1b) with various aromatic acids as acylating agents. All of these esters were tested against 14 different human cancer cell lines. The antitumor activity of these compounds was related to the nature of the substituting groups of their side aromatic chains. In general, esters with strong electron-withdrawing groups on their side aromatic chains … Show more

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Cited by 5 publications
(4 citation statements)
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“…The synthesis of compound 1 has been described elsewhere. 21,22 Briefly, 206 mg (1 mmol) α-lipoic acid was dissolved in 10 mL dried dichloromethane, and 227 mg (1.1 mmol) DCC was added and stirred at room temperature for 30 min. Then, 150 mg (1 mmol) of acetaminophen and 18 mg (0.15 mmol) of DMAP were added and stirred at room temperature for 3 h. The precipitate was removed by filtration, and the filtrate was washed three times with water, 5% acetic acid solution, and then dried over anhydrous sodium sulfate overnight.…”
Section: Synthesis Of H 2 S Donorsmentioning
confidence: 99%
“…The synthesis of compound 1 has been described elsewhere. 21,22 Briefly, 206 mg (1 mmol) α-lipoic acid was dissolved in 10 mL dried dichloromethane, and 227 mg (1.1 mmol) DCC was added and stirred at room temperature for 30 min. Then, 150 mg (1 mmol) of acetaminophen and 18 mg (0.15 mmol) of DMAP were added and stirred at room temperature for 3 h. The precipitate was removed by filtration, and the filtrate was washed three times with water, 5% acetic acid solution, and then dried over anhydrous sodium sulfate overnight.…”
Section: Synthesis Of H 2 S Donorsmentioning
confidence: 99%
“…Several additional new camptothecin derivatives have been synthesized and tested pre-clinically and clinically. In our laboratory, various camptothecin were synthesized esters for biological evaluation (7)(8)(9)(10). Crystalline camptothecin-20-O-propionate hydrate (CZ48) was prepared using an acid-catalyzed method with a high reaction yield (11).…”
Section: Introductionmentioning
confidence: 99%
“…In order to find better CPT analogues for biological evaluation, we have synthesized and tested various CPT ester derivatives in our laboratory (23)(24)(25)(26). Among these ester compounds, CZ48 (a C20-propionate ester of CPT) has demonstrated strong anticancer activity against human tumor xenografts grown in nude mice with an exceptional lack of toxicity (27).…”
Section: Introductionmentioning
confidence: 99%