Synthesis and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines of Thieno[2,3-d]pyrimidine Derivatives Containing Isoxazole Moiety

Yong, Jianping; Lu, Canzhong; Wu, Xiao‐Yuan

doi:10.20944/preprints201703.0190.v1

Cited by 2 publications

(3 citation statements)

References 5 publications

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“…The cytotoxicity data revealed that compound 184 (Figure 26; IC 50 : 18.87 ± 0.2 μg/ml) with chloro substitution on the phenyl ring displayed the highest cytotoxicity against the MCF‐7cell line, while the compound 185 (Figure 26; IC 50 : 40.74 ± 1.7 μg/ml) with unsubstituted phenyl ring showed the maximum cytotoxicity against HeLa cell line 231 . In 2018, Yong et al, 232 worked on the synthesis of thienopyrimidine containing the isoxazole template. They screened their anticancer efficacy taking gefitinib as a reference standard.…”

Section: Introductionmentioning

confidence: 97%

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Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update

Laxmikeshav

Kumari

Shankaraiah

2021

Medicinal Research Reviews

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This review article proposes a comprehensive report of the design strategies engaged in the development of various sulfur-bearing cytotoxic agents. The outcomes of various studies depict that the sulfur heterocyclic framework is a fundamental structure in diverse synthetic analogs representing a myriad scope of therapeutic activities. A number of five-, six-and seven-membered sulfur-containing heterocyclic scaffolds, such as thiazoles, thiadiazoles, thiazolidinediones, thiophenes, thiopyrans, benzothiazoles, benzothiophenes, thienopyrimidines, simple and modified phenothiazines, and thiazepines have been discussed. The subsequent studies of the derivatives unveiled their cytotoxic effects through multiple mechanisms (viz. inhibition of tyrosine kinases, topoisomerase I and II, tubulin, COX, DNA synthesis, and PI3K/Akt and Raf/MEK/ERK signaling pathways), and several others. Thus, our concise illustration explains the design strategy and anticancer potential of these five-and six-membered sulfur-containing heterocyclic molecules along with a brief outline on seven-membered sulfur heterocycles. The thorough assessment of antiproliferative activities with the reference drug allows a proficient assessment of the structure-activity relationships (SARs) of the diversely synthesized molecules of the series.

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Section: Introductionmentioning

confidence: 97%

“…Amongst the analogs, compound 186 was found to show the maximum potency towards A549, HCT116, and MCF‐7 cell lines (Table 9). Thus, this molecule can be considered as a potential drug lead for the advancement of antitumor drugs 232 …”

Section: Introductionmentioning

confidence: 99%

Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update

Laxmikeshav

Kumari

Shankaraiah

2021

Medicinal Research Reviews

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“…14 In addition, other heterocycles such as isoxazole derivatives were said to be powerful anticancer EGFR-TKIs. For example, the isoxazole derivative IV (Figure 1) was very good at inhibiting cancer cells proliferation, 15 and the isoxazole derivatives V were good at inhibiting cancer cells expressing EGFR-TK (Figure 1). 16 In the same way, 1,2,4-oxadiazole is the only oxadiazole that can be found in natural products.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Indole-Oxadiazole coupled isoxazole hybrids as potent EGFR targeting anticancer agents

Dubba,

Kumar Koppula

2024

CBL

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The synthesis of new indole-oxadiazole coupled isoxazole hybrids (6a-o) synthesized by the Cu(I)-catalyzed reaction of in situ generated nitrile oxides with 3-(3,5-dichloro-4-methoxyphenyl)-5-(1-(prop-2-yn-1-yl)-1H-indol-3-yl)-1,2,4-oxadiazole in good yields have been reported here. The chemical structures of all newly synthesized hybrids were confirmed by 1 H-NMR, 13 C-NMR, and Mass spectra. All synthesized compounds were screened for their in vitro cytotoxicity against two breast cancer cell lines MCF-7 and MDA-MB-231 respectively. All the derivatives were more active against MCF7 than MDA-MB-231 cancer cells and few compounds showed better activity than the standard erlotinib. The ability of more potent compounds to inhibit EGFR tyrosine kinase, one of the key enzymes involved in breast carcinomas was evaluated by in vitro enzymatic assay and it was found that the compound (6g) and (6m) had more inhibitory activity IC50 values 0.311±0.05 and 0.203±0.03 µM than erlotinib (IC50=0.421±0.03 µM).

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Synthesis and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines of Thieno[2,3-d]pyrimidine Derivatives Containing Isoxazole Moiety

Abstract: Abstract：Under the guidance of our previous achievements, and in order to extend this small molecular library. In current work, other 21 novel structures of

Cited by 2 publications

References 5 publications

Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update

Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update

Synthesis of Indole-Oxadiazole coupled isoxazole hybrids as potent EGFR targeting anticancer agents

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