Synthesis, Antitumor and Anti-inflammatory Activities of 2-thienyl-3-substitued Indole Derivatives
نویسندگان
چکیده
A series of 2-thienyl-3-substitued indole derivatives (1-11) were synthesized. Their structures were established on the basis of elemental and spectral (IR, HNMR and Mass spectral data) studies. All the 1 synthesized compounds have been tested for their antitumor activity against breast cancer cell line (MCF-7) using doxorubicin as a standard drug (IC =2.97 μg/ml). Most of the prepared compounds showed good to 50 moderate antitumor activity. The most potent one was 10b ( IC =2.6 μg/ml). Twelve of the prepared compounds 50 were evaluated for their anti-inflammatory activity (against carrageenan induced oedema in albino rats at a dose of 50 mg/kg body weight using indomethacin at a dose of 25mg/kg body weight as a standard drug) and ulcerogenic effect. Compound 9a exhibited 55.31% inhibition with ulcerogenic activity less than that of indomethacin.
منابع مشابه
Anti-inflammatory and analgesic activities of some newly synthesized pyridinedicarbonitrile and benzopyranopyridine derivatives.
In continuation of our search for new substituted pyridine based anti-inflammatories, reaction of 1-(2-thienyl or furanyl)-3-(2-hydroxyphenyl)-2-propen-1-ones (1) with malononitrile in alcoholic KOH solution afforded a mixture of 4-alkoxy-2-(2-thienyl or furanyl)-5H-[1]benzopyrano[3,4-c]pyridine-5-ones (2) and 2-alkoxy-4-amino-6- (2-thienyl or furanyl)-3,5-pyridinedicarbonitriles (3). Some of t...
متن کاملSynthesis and Anti-inflammatory Activity of Indole Derivatives
The present investigation is concerned with synthesis of new substituted indole derivatives 1-39 with the objective of discovering novel and potent anti-inflammatory agent. The structure of all the synthesized compounds were elucidated by spectral (IR, HNMR and mass) and elemental (C, H, N) analysis. The obtained compounds were screened for their anti-inflammatory as well as analgesic activitie...
متن کاملThiamine hydrochloride (vitamin B1) as an efficient catalyst for the synthesis of 4-(3H)-Quinazolinone derivatives using grinding method.
Herein we explore facile synthesis of 4-(3H)-Qunazolinone derivatives, achieved by the cyclocondensation of anthranilic acid, aromatic amines and triethyl orthoformate in presence of thiamine hydrochloride (Vitamin B1) as a catalyst, using grinding method. This protocol offers several advantages such as reusability of catalyst, excellent yield, shorter reaction time and economic availability.Qu...
متن کاملThiamine hydrochloride (vitamin B1) as an efficient catalyst for the synthesis of 4-(3H)-Quinazolinone derivatives using grinding method.
Herein we explore facile synthesis of 4-(3H)-Qunazolinone derivatives, achieved by the cyclocondensation of anthranilic acid, aromatic amines and triethyl orthoformate in presence of thiamine hydrochloride (Vitamin B1) as a catalyst, using grinding method. This protocol offers several advantages such as reusability of catalyst, excellent yield, shorter reaction time and economic availability.Qu...
متن کاملSynthesis, Characterization and Anti-Inflammatory Activity of Some 1, 3,4 -Oxadiazole Derivatives
A series of five-membered heterocyclic rings were synthesized by the reaction between benzoyl chloride and various chlolro-nitro-benzoyl chlorides and semi carbazide to form (C1-C7) compounds and was tested for their anti-inflammatory activity determined by rat-paw-oedema method. All the synthesis compounds have been characterized by 1HNMR, IR and Mass spectral data. The compounds were purified...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
دوره شماره
صفحات -
تاریخ انتشار 2013