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Journal of the Korean Chemical Society (JKCS)

ISSN 1017-2548(Print)
ISSN 2234-8530(Online)
Volume 53, Number 1
JKCSEZ 53(1)
February 20, 2009 

Synthesis of Hydrazone Derivatives of 4-(2-Chloroethyl) semicarbazide : A New Class of Cytotoxic Agents

4-(2-Chloroethyl) semicarbazide의 히드라존 유도체 합성:새로운 종류의 세포독성요법제
O I El Sabbagh*, M E El Sadek, M E Aboukull, H M Shallal

O I El Sabbagh*, M E El Sadek, M E Aboukull, H M Shallal
히드라존, 2-(Chloroethyl)요소들, 4-(2-Chloroethyl) semicarbazides, 세포독성요법 활성 , Hydrazones, 2-(Chloroethyl)ureas, 4-(2-Chloroethyl) semicarbazides, Cytotoxic activity
새로운 종류의 히드라존 유도체는 4-(2-chloroethyl) semicarbazides로 부터 합성되었고, 인간 두 뇌(U251)와 간(Hepg2)의 암세포 에 대해 항증식성을 보였다. 히드라존 화합물은 벤즈알데히드, 아세토 페논, 3-formylindole 유도체이다. 아세토페논 유도체중에 3e (p-methoxy substituted)와 and 3f (p-nitro substituted)는 Hepg2 세포 (각각IC50 = 6 ,8 μg/mL) 에 대해 가장 높은 세포독성활성을 보인다. 3-Formylindole 유도체중에 4a (hydrazone of 3-formylindole)은 U251 (IC50 = 21 μg/mL)와 Hepg2 (IC50 = 7 μg/mL)에 강한 세포독성활성을 보인다.

A new series of hydrazone derivatives were synthesized from 4-(2-chloroethyl)semicarbazide and their antiproliferative activity against human brain (U251) and liver (Hepg2) carcinoma cell lines were evaluated. The hydrazone compounds are benzaldehyde (2a-2g), acetophenone (3a-3f), and 3-formylindole derivatives (4a-4d). Among the acetophenone derivatives, 3e (p-methoxy substituted) and 3f (p-nitro substituted) showed the highest cytotoxic activity against Hepg2 cell line (IC50 = 6 and 8 μg/ml, respectively). Among the 3-formylindole derivatives, 4a (hydrazone of 3-formylindole itself) showed a pronounced cytotoxic activity against both U251 (IC50 = 21 μg/ml) and Hepg2 (IC50 = 7 μg/ml).

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