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T1 - Synthesis and antitumor activity of tropolone derivatives. 5

Adel S, Azab E, Mohamed A, Omar A, Alaa AM, Naglaa I, et al. Design, synthesis and biological evaluation of novel quinazoline derivatives as potential antitumor agents: Molecular docking study. Eur J Med Chem 2010; 45:4188-98.

T1 - Synthesis, characterization, and antitumor activity of 5-iodouracil complexes

Triazole anlogs of benzothiazole (2.35) were synthesized and screened for anti-tubercular activity against M. tuberculosis H37Rv strain and antimicrobial activity against some Gram positive and negative bacteria and fungal species. The 4-Cl analogue with MIC 25 µg/ml was revealed better anti-tubercular agent than Rifampicin (MIC 40 µg/ml) 78.

Synthesis and antitumor activity of 4 ..

T1 - Design and synthesis of benzothiazole schiff bases of potential antitumor activity

Recently, heterocyclic compounds analogues and their derivatives have attracted strong interest in medicinal chemistry due to their biological and pharmacological properties. The small and simple benzothiazole nucleus possesses numerous biological properties like - antitumor, antimicrobial, anti-inflammatory, anticonvulsant, and antidiabetic activities. These activities are also possessed by its substituted derivatives as well. The present review focuses on some commonly used easy procedures to synthesize the benzothiazole moiety and its derivatives, which comprise of different biological activities.

Due to these biological activities, the synthesis of benzothiazole is a considerable area of current discussion. The classical method involves condensation of o-aminothiophenols with substituted aldehydes 8-14, acyl chlorides, carboxylic acids 15-16 or esters, nitriles 17. Other most commonly used methods include Pd/Cu/Mn/chloranil catalyzed cyclization of o-halothioformanilides 18-22. The survey of literature related to benzothiazoles reveals the presence of this bicyclic ring system in various amine or terrestrial natural compounds, which have useful biological properties 23. Benzothiazole derivatives possess a wide spectrum of biological applications such as antitumor 26-52, antimicrobial 54-83, schictosomicidal 84, anti-inflammatory 85-93, anticonvulsants 94-102, antidiabetic 103-108, antipsychotic 109 and diuretic 111 etc.

Synthesis, antitumor activity evaluation, and DNA …

T1 - Synthesis and antitumor activity of some substituted indazole derivatives

AB - A new series of 7-fluoro-6-(4-methyl-1-piperazinyl)-2-(thiosubstituted)- 4(3H)-quinazolinones was synthesized as potential antitumor agents by multi-step synthesis starting with the commercially available 3-chloro-4-fluoroaniline. The most promising candidate, 7-fluoro-6-(4-methyl-1-thyl-1-piperazinyl)-2- thioethyl-4(3H)-quinazolinone (5a), was screened in 60 human cancer cells by NCI.

2-m-Azidobenzoyl and 2-m-chlorobenzoyl baccatin III analogs were prepared from taxinine, a major component in Japanese yew leaves. In this study, a novel acetyl migration from 13- to 4-hydroxyl group was observed. The antitumor activity of these compounds was evaluated.

T1 - Synthesis and antitumor activity of podophyllotoxin aza-analogues
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Synthesis of FR901464 and analogs with antitumor activity

A new series of 7-fluoro-6-(4-methyl-1-piperazinyl)-2-(thiosubstituted)- 4(3H)-quinazolinones was synthesized as potential antitumor agents by multi-step synthesis starting with the commercially available 3-chloro-4-fluoroaniline. The most promising candidate, 7-fluoro-6-(4-methyl-1-thyl-1-piperazinyl)-2- thioethyl-4(3H)-quinazolinone (5a), was screened in 60 human cancer cells by NCI.

Photo-induced synthesis and in vitro antitumor activity …

N2 - A new series of 7-fluoro-6-(4-methyl-1-piperazinyl)-2-(thiosubstituted)- 4(3H)-quinazolinones was synthesized as potential antitumor agents by multi-step synthesis starting with the commercially available 3-chloro-4-fluoroaniline. The most promising candidate, 7-fluoro-6-(4-methyl-1-thyl-1-piperazinyl)-2- thioethyl-4(3H)-quinazolinone (5a), was screened in 60 human cancer cells by NCI.

SYNTHESIS AND ANTITUMOR ACTIVITY OF 5-BROMO …

As part of a study on the structure-activity relationship of antitumor-active tropolone derivatives, a series of bistropone analogues, related to potently active bistropolone 1a, were synthesized and tested for their antitumor activity in in vitro (KB cell) and in vivo (leukemia P388 in mice) systems. The methoxytropones 3 and 5, hydroxytropothione 10, and (N-methylamino)tropones 12 and 13 were inactive in both systems. Methoxytropone 6 exhibited weak activity, whose potency was equal to that of monotropolone 2a.

Synthesis and antitumor activity of tetrandrine derivatives.

AB - Uracil and thymine α-methylene-γ-lactones and related derivatives have been synthesized as novel potential alkylating antitumor agents. The synthesis of these compounds involved the convenient Reformatsky-type reaction between ethyl α-(bromomethyl)acrylate and the proper pyrimidinyl ketones. Preliminary in vivo tumor assay indicated that these compounds were active against the Walker 256 carcinosarcoma in rats and the P-388 lymphocytic leukemia as well as the B-16 melanotic melanoma in mice at 2.5-25 mg/kg.

Synthesis and evaluation of antitumor activity of 2- and …

N2 - 2-m-Azidobenzoyl and 2-m-chlorobenzoyl baccatin III analogs were prepared from taxinine, a major component in Japanese yew leaves. In this study, a novel acetyl migration from 13- to 4-hydroxyl group was observed. The antitumor activity of these compounds was evaluated.

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