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Journal of the Korean Chemical Society (JKCS)

ISSN 1017-2548(Print)
ISSN 2234-8530(Online)
Volume 41, Number 7
JKCSEZ 41(7)
February 20, 1997 

 
Title
Syntheses and in vitro Antitumor Activities of 8-Azaxanthine and Its Derivatives

8-Azaxanthine과 그 유도체의 합성 및 시험관내 항암 활성
Author
Bong-Hun Lee*, Jung-Hee Shin, Tae-Sik Jang, Jang-Su Park, Shin-Won Kang

이봉훈,신정희,장태석,박장수,강신원
Keywords
Abstract
8-Azaxanthine (1), 3-β-D-ribofuranosyl-8-azaxanthine (2), 3-β-D-ribofuranosyl-8-azaxanthine-5'-monophosphate (3), 그리고 3-β-D-ribofiranosyl-8-azaxanthine-5'-(3-pyridinylcarbonyl)monophosphate (4)를 합성한 후 mouse leukemia P788, Murine mammary carcinoma FM34, Human histiocytic lymphoma U937 암세포들에 대해 시험관내 항암활성을 MTT를 이용한 방법으로 예측하고 IC5o(μmol/mI)으로 나타내었다. 그 결과, 비정상적인 염기의 N-3와 당의 C-1' glycoside 결합을 가진 2는 세가지의 암세포에 대해 감수성이 좋아 IC50이 각각0.05, 0.06, 0.06 μmol/mI이었으나 항세균 활성 예측에서는 감수성을 보이지 않았다. Human histiocytic lymphoma U937 세포에 대한 IC50은 1이 0.33, 2는 0.06, 3은 0.25, 그리고 4는 0.33 μmol/mL로 구조 변화에 따라 서로 다른 값을 보였다.

8-Azaxanthine (1), 3-β-D-ribofuranosyl-8-azaxanthine (2), 3-β-D-ribofuranosyl-8-azaxanthine-5'-monophosphate (3), and 3-β-D-ribofiranosyl-8-azaxanthine-5'-(3-pyridinylcarbonyl)monophosphate (4) were synthesized. The in vitro antitumor activities of the synthesized compounds against P388 mouse leukemia, FM3A mammary carcinoma, and U937 human histiocytic lymphoma cells were determined by MTT assay. 2 with unnatural N-3 and C-1' glycoside bond had activity against three tumor cell lines and IC50 s of these compounds were 0.05, 0.06, and 0.06 μmol/mL against three tumor cell lines, respectively. But these compounds had no antibacterial activity. IC50 s against U937 human histiocytic lymphoma cells were verified with the structural modification: IC50s of 1, 2, 3, and 4 were 0.33, 0.06, 0.25, and 0.33μmol/mL, respectively.

Page
357 - 361
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