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Literature DB >> 23524379

A structure-activity relationship study on multi-heterocyclic molecules: two linked thiazoles are required for cytotoxic activity.

Seong Jong Kim¹, Chun Chieh Lin, Chung-Mao Pan, Dimple P Rananaware, Deborah M Ramsey, Shelli R McAlpine.

Abstract

We report the synthesis, cytotoxicity, and phenotypic analysis of oxazole and thiazole containing fragments. Evaluating the optimal size and heterocycle for growth inhibition and apoptosis showed that activity required at least two thiazoles sequentially connected. This is the first detailed comparison of biological activity between multi-heterocyclic containing fragments.

Entities: CellLine Chemical Disease Gene

Year: 2012 PMID： 23524379 PMCID： PMC3601786 DOI： 10.1039/C2MD20291C

Source DB: PubMed Journal: Medchemcomm ISSN： 2040-2503 Impact factor: 3.597

31 in total

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Review 4. From amino acids to heteroaromatics--thiopeptide antibiotics, nature's heterocyclic peptides.

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5. Discovery of a series of phosphonic acid-containing thiazoles and orally bioavailable diamide prodrugs that lower glucose in diabetic animals through inhibition of fructose-1,6-bisphosphatase.

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Review 7. Pharmacological and therapeutic properties of ritonavir-boosted protease inhibitor therapy in HIV-infected patients.

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A structure-activity relationship study on multi-heterocyclic molecules: two linked thiazoles are required for cytotoxic activity.

Review 1. The morphology of apoptosis.

2. Planar-Chiral Heterocycles as Ligands in Metal-Catalyzed Processes: Enantioselective Addition of Organozinc Reagents to Aldehydes.

Review 3. Ixabepilone for the treatment of solid tumors: a review of clinical data.

Review 4. From amino acids to heteroaromatics--thiopeptide antibiotics, nature's heterocyclic peptides.

5. Discovery of a series of phosphonic acid-containing thiazoles and orally bioavailable diamide prodrugs that lower glucose in diabetic animals through inhibition of fructose-1,6-bisphosphatase.

6. Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach.

Review 7. Pharmacological and therapeutic properties of ritonavir-boosted protease inhibitor therapy in HIV-infected patients.

Review 8. Cyanobactins-ribosomal cyclic peptides produced by cyanobacteria.

9. Progress towards the synthesis of Urukthapelstatin A and two analogues.

Review 10. Apoptosis: a basic biological phenomenon with wide-ranging implications in tissue kinetics.

1. RITA Mimics: Synthesis and Mechanistic Evaluation of Asymmetric Linked Trithiazoles.