Synthesis and biological evaluation of peptidomimetics containing the tryptamine moiety as a potential antitumor agent

Wang, Xiaohui; Su, Haihuan; Chen, Changshui; Cao, Xiufang

doi:10.1039/c4ra16949b

Cited by 7 publications

(2 citation statements)

References 22 publications

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“…In another recent study on triazole-linked 1,4-dihydropyridine-isatin scaffolds (N1, N2, N13), the IC 50 values were evaluated as 13.66, 6.73, and 19.36 µM, respectively, for the same cell line [45]. The extract of Isatis indigotica leaves and indole alkaloids (Ih, Ij) were tested on the same cell line and the IC 50 values were reported as 58 µM [46] and 4.88 ± 0.78 and 6.60 ± 1.20 [47], respectively. The IC 50 values evaluated for isatin derivatives in current studies have been low compared to the literature cited above, especially for the compound IST-02.…”

Section: Cytotoxicity Analysis By Cell Line Studiesmentioning

confidence: 99%

Investigations on Anticancer Potentials by DNA Binding and Cytotoxicity Studies for Newly Synthesized and Characterized Imidazolidine and Thiazolidine-Based Isatin Derivatives

et al. 2022

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Imidazolidine and thiazolidine-based isatin derivatives (IST-01–04) were synthesized, characterized, and tested for their interactions with ds-DNA. Theoretical and experimental findings showed good compatibility and indicated compound–DNA binding by mixed mode of interactions. The evaluated binding parameters, i.e., binding constant (Kb), free energy change (ΔG), and binding site sizes (n), inferred comparatively greater and more spontaneous binding interactions of IST-02 and then IST-04 with the DNA, among all compounds tested under physiological pH and temperature (7.4, 37 °C). The cytotoxic activity of all compounds was assessed against HeLa (cervical carcinoma), MCF-7 (breast carcinoma), and HuH-7 (liver carcinoma), as well as normal HEK-293 (human embryonic kidney) cell lines. Among all compounds, IST-02 and 04 were found to be cytotoxic against HuH-7 cell lines with percentage cell toxicity of 75% and 66%, respectively, at 500 ng/µL dosage. Moreover, HEK-293 cells exhibit tolerance to the increasing drug concentration, suggesting these two compounds are less cytotoxic against normal cell lines compared to cancer cell lines. Hence, both DNA binding and cytotoxicity studies proved imidazolidine (IST-02) and thiazolidine (IST-04)-based isatin derivatives as potent anticancer drug candidates among which imidazolidine (IST-02) is comparatively the more promising.

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Section: Cytotoxicity Analysis By Cell Line Studiesmentioning

confidence: 99%

Investigations on Anticancer Potentials by DNA Binding and Cytotoxicity Studies for Newly Synthesized and Characterized Imidazolidine and Thiazolidine-Based Isatin Derivatives

et al. 2022

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“…Recently, during the course of our research for high active compounds, three series of novel peptidomimetics bearing natural tryptamine moiety were designed, synthesized, and evaluated for their inhibition activities against cell proliferation 20 . Some of the prepared compounds exhibited significant inhibition activities against human hepatoma cancer (HepG2 and Huh-7), human melanoma (A875) cell lines compared with the control 5-fluorouracil.…”

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confidence: 99%

Peptidomimetics Based On Dehydroepiandrosterone Scaffold: Synthesis, Antiproliferation Activity, Structure-Activity Relationship, and Mechanisms

Wang

et al. 2016

Sci Rep

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A series of novel peptidomimetics bearing dehydroepiandrosterone moiety were designed, synthesized, and evaluated for their inhibition activities against cell proliferation. According to the preliminary studies on inhibitory activities, some of the newly prepared compounds indicated significantly inhibition activities against human hepatoma cancer (HepG2), human lung cancer (A549), human melanoma (A875) cell lines compared with the control 5-fluorouracil. Especially, compounds Ii (IC50 < 14 μM) and Ik (IC50 < 13 μM) exhibited obvious inhibition activities against all tested cell lines. The highly potential compound Ik induced apoptosis in HepG2 cells were analyzed by flow cytometry, and the apoptotic effects of compound Ik were further evaluated using Annexin V-FITC/propidium iodide dual staining assay, which revealed these highly potential compounds induced cell death in HepG2 cells at least partly by apoptosis.

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Development of Fused and Substituted Pyrimidine Derivatives as Potent Anticancer Agents (A Review)

Abbas¹,

Swamy²,

Dhiwar³

et al. 2021

Pharm Chem J

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Synthesis and biological evaluation of peptidomimetics containing the tryptamine moiety as a potential antitumor agent

Abstract: A series of novel peptidomimetics bearing tryptamine moiety were designed, synthesized, and evaluated for their inhibition activities against cell proliferation (HepG2, Huh-7, A875 and BEL-7402/5-FU cell lines).

Cited by 7 publications

References 22 publications

Investigations on Anticancer Potentials by DNA Binding and Cytotoxicity Studies for Newly Synthesized and Characterized Imidazolidine and Thiazolidine-Based Isatin Derivatives

Investigations on Anticancer Potentials by DNA Binding and Cytotoxicity Studies for Newly Synthesized and Characterized Imidazolidine and Thiazolidine-Based Isatin Derivatives

Peptidomimetics Based On Dehydroepiandrosterone Scaffold: Synthesis, Antiproliferation Activity, Structure-Activity Relationship, and Mechanisms

Development of Fused and Substituted Pyrimidine Derivatives as Potent Anticancer Agents (A Review)

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