Hybrid pharmacophore design and synthesis of isatin–benzothiazole analogs for their anti-breast cancer activity

Solomon, V. Raja; Hu, Changkun; Lee, Hoyun

doi:10.1016/j.bmc.2009.08.068

Cited by 226 publications

(106 citation statements)

References 27 publications

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“…26 Isatin-benzothiazole Schiff base derivatives have shown anticancer activity in breast tumor cell lines. 27 Here, we report the discovery of isatin Mannich and Schiff base derivatives (IMSBDs) that activate the p53 transcription factor. These compounds were identified by in silico screening (Table S2), and their activities were validated in cellulo using a human bone osteosarcoma epithelial U2OS cell line, which stably expressed a p53-driven enhanced green fluorescent protein (EGFP) reporter.…”

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confidence: 99%

Discovery of Novel Isatin-Based p53 Inducers

Davidovich

Aksenova

Petrova

et al. 2015

ACS Med. Chem. Lett.

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A series of isatin Schiff base derivatives were identified during in silico screening of the small molecule library for novel activators of p53. The compounds selected based on molecular docking results were further validated by a high-content screening assay using U2OS human osteosarcoma cells with an integrated EGFP-expressing p53-dependent reporter. The hit compounds activated and stabilized p53, as shown by Western blotting, at higher rates than the well-known positive control Nutlin-3. Thus, the p53-activating compounds identified by this approach represent useful molecular probes for various cancer studies.KEYWORDS: in silico, isatin Mannich and Schiff bases, p53 activators, in vivo assay, protein−protein interactions, MDM2

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confidence: 99%

Discovery of Novel Isatin-Based p53 Inducers

Davidovich

Aksenova

Petrova

et al. 2015

ACS Med. Chem. Lett.

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“…2) [22]. Although chemotherapy is widely recognized as the mainstay of cancer therapy, undesirable side effects limited the use of anticancer drugs in chemotherapeutics [23].…”

Section: Benzopyran and Breast Cancermentioning

confidence: 99%

“…Sashidhara et al synthesized coumarin-monastrol hybrid (23) and reported it as an anti-breast cancer agent. It was found that hybrid (23) was effective in breast cancer cells (MCF-7 and MDA-MB-231).…”

Section: Caspase-3 Activationmentioning

confidence: 99%

A Review of Benzopyran Derivatives in Pharmacotherapy of Breast Cancer

Kumar

Singh

Azizur

et al. 2018

Asian J Pharm Clin Res

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One of the naturally occurring compounds containing oxygen moiety is benzopyran. Depending on its substitution pattern, different biological effects are shown. The benzopyran ring system is present in many natural products (such as genistein, hesperidin, and warfarin) as well as synthetic products. It displays pharmacological properties such as antitumor, anti-HIV, antimicrobials, anti-inflammatory, and anticoagulants. The sufficient literature support and the fact that benzopyran has potential as a pharmacophore particularly as anti-breast cancer, etc, current research seemed pertinent keeping in view the mechanism of anti-breast cancer activity. Therefore, the objective of this review is to focus on important benzopyran analogs with anti-breast cancer activity and highlight their mechanisms of action.

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“…Over the years, molecular hybridization based drug design approach [13,14] has been exploited by many researchers in order to develop some promising new hybrid chemical entities (NHCEs), displaying significant therapeutic values. The combination of two pharmacophores into a single molecular skeleton is a well established approach for designing more potent drugs with significant increase in activity.…”

Section: Introductionmentioning

confidence: 99%

One-Pot Synthesis of Some Novel N-Aryl-1,4-Dihydropyridines Derivatives Bearing Nitrogen Mustard

Singala

Shah

2015

ILCPA

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The synthesis of a novel dihydropyridine, bearing carbethoxy groups at C(3) and C(5), respectively, has been achieved by applying three component Hantzsch-type condensation. The products were assayed for their in vitro biological assay antibacterial activity against with two Gram-positive bacteria Staphylococcus aureus MTCC-96, Streptococcus pyogenes MTCC 443, two Gram-negative bacteria Escherichia coli MTCC 442, Pseudomonas aeruginosa MTCC 441 and three fungal strains Candida albicans MTCC 227, Aspergillus Niger MTCC 282, Aspergillus clavatus MTCC 1323 taking ampicillin, chloramphenicol, ciprofloxacin, norfloxacin, nystatin, and griseofulvin as standard drugs.

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Hybrid pharmacophore design and synthesis of isatin–benzothiazole analogs for their anti-breast cancer activity

Cited by 226 publications

References 27 publications

Discovery of Novel Isatin-Based p53 Inducers

Discovery of Novel Isatin-Based p53 Inducers

A Review of Benzopyran Derivatives in Pharmacotherapy of Breast Cancer

One-Pot Synthesis of Some Novel N-Aryl-1,4-Dihydropyridines Derivatives Bearing Nitrogen Mustard

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