Design, synthesis, anticancer activity and mechanism studies of novel 2-amino-4-aryl-pyrimidine derivatives of ursolic acid

2022 ◽  
Author(s):  
Wen-Yan Wang ◽  
Zihui Yang ◽  
A-Liang Li ◽  
Qing-Song Liu ◽  
Yue Sun ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Ursolic Acid ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Pyrimidine Derivatives ◽  
Design Synthesis ◽  
Derivatives Of ◽  
Mcf 7

A series of novel 2-amino-4-aryl-pyrimidine derivatives of ursolic acid were designed, synthesized, and evaluated for their anticancer activities against four cancer cell lines (MCF-7, HeLa, HepG2, and A549) and a...

Design, Synthesis and Anticancer Activity of 4-Morpholinothieno[3,2-D]-Pyrimidine Derivatives Bearing Chromone Moiety

2014 ◽  
Vol 989-994 ◽  
pp. 568-571 ◽  
Author(s):  
Cheng Yu Sun ◽  
Chen Chen ◽  
Chun Jiang Wu ◽  
Peng Wu Zheng ◽  
Wu Fu Zhu
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
High Selectivity ◽  
Cancer Cell Lines ◽  
Inhibition Rate ◽  
Pyrimidine Derivatives ◽  
Design Synthesis ◽  
H Nmr

A series of 4-morpholinothieno [3,2-d] pyrimidine derivatives containing chromone moiety (5a-5e) were synthesized and their structures were confirmed by 1H NMR and MS spectrum. The synthesized compounds were evaluated for their cytotoxicity against three cancer cell lines (PC-3, H460, SGC-7901). Two of them exhibited moderate cytotoxicity and high-selectivity against one or more cell lines. At 10μM levels, the inhibition rate of compound 5c against SGC-7901 cell lines was 58.9%, and that of compound 5d against PC-3 cell lines was 56.4%.

scholarly journals Design, Synthesis and Cytotoxic Evaluation of Novel Lupane Triterpenoid and Ursolic Acid Derived 2-Aminobenzamides

2018 ◽  
Vol 13 (7) ◽  
pp. 1934578X1801300
Author(s):  
Dang Thi Tuyet Anh ◽  
Dinh Thi Cuc ◽  
Le Nhat Thuy Giang ◽  
Nguyen Thi Hien ◽  
Vu Ngoc Doan ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Ursolic Acid ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Cytotoxic Agents ◽  
Design Synthesis

Series of novel triterpenoid hybrids were designed and synthesized by introducing 2-aminobenzamide moiety at C28 position of triterpenoid derivatives. Thirteen new conjugates were thus successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity in KB and HepG2 cancer cell lines.

scholarly journals Novel Papaverine Metal Complexes with Potential Anticancer Activities

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5447
Author(s):  
Ahmed Gaber ◽  
Walaa F. Alsanie ◽  
Deo Nandan Kumar ◽  
Moamen S. Refat ◽  
Essa M. Saied
Keyword(s):  
Breast Cancer ◽  
Biological Activity ◽  
Metal Complexes ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Mcf 7

Cancer is one of the leading causes of death worldwide. Although several potential therapeutic agents have been developed to efficiently treat cancer, some side effects can occur simultaneously. Papaverine, a non-narcotic opium alkaloid, is a potential anticancer drug that showed selective antitumor activity in various tumor cells. Recent studies have demonstrated that metal complexes improve the biological activity of the parent bioactive ligands. Based on those facts, herein we describe the synthesis of novel papaverine–vanadium(III), ruthenium(III) and gold(III) metal complexes aiming at enhancing the biological activity of papaverine drug. The structures of the synthesized complexes were characterized by various spectroscopic methods (IR, UV–Vis, NMR, TGA, XRD, SEM). The anticancer activity of synthesized metal complexes was evaluated in vitro against two types of cancer cell lines: human breast cancer MCF-7 cells and hepatocellular carcinoma HepG-2 cells. The results revealed that papaverine-Au(III) complex, among the synthesized complexes, possess potential antimicrobial and anticancer activities. Interestingly, the anticancer activity of papaverine–Au(III) complex against the examined cancer cell lines was higher than that of the papaverine alone, which indicates that Au-metal complexation improved the anticancer activity of the parent drug. Additionally, the Au complex showed anticancer activity against the breast cancer MCF-7 cells better than that of cisplatin. The biocompatibility experiments showed that Au complex is less toxic than the papaverine drug alone with IC50 ≈ 111 µg/mL. These results indicate that papaverine–Au(III) complex is a promising anticancer complex-drug which would make it a suitable candidate for further in vivo investigations.

scholarly journals Design, Synthesis, and Antitumor Activity of Olmutinib Derivatives Containing Acrylamide Moiety

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 3041
Author(s):  
Xiaohan Hu ◽  
Sheng Tang ◽  
Feiyi Yang ◽  
Pengwu Zheng ◽  
Shan Xu ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antitumor Agents ◽  
Cancer Cell Lines ◽  
Design Synthesis ◽  
Structure Activity ◽  
Excellent Activity ◽  
Ic50 Values ◽  
Mcf 7

Two series of olmutinib derivatives containing an acrylamide moiety were designed and synthesized, and their IC50 values against cancer cell lines (A549, H1975, NCI-H460, LO2, and MCF-7) were evaluated. Most of the compounds exhibited moderate cytotoxic activity against the five cancer cell lines. The most promising compound, H10, showed not only excellent activity against EGFR kinase but also positive biological activity against PI3K kinase. The structure–activity relationship (SAR) suggested that the introduction of dimethylamine scaffolds with smaller spatial structures was more favorable for antitumor activity. Additionally, the substitution of different acrylamide side chains had different effects on the activity of compounds. Generally, compounds H7 and H10 were confirmed as promising antitumor agents.

scholarly journals Design and Evaluation of Licochalcone A Derivatives as Anticancer Agents

2018 ◽  
Vol 13 (6) ◽  
pp. 1934578X1801300
Author(s):  
Goo Yoon ◽  
Seung Hoon Cheon ◽  
Jung Hyun Shim ◽  
Seung Sik Cho
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Licochalcone A ◽  
Lead Compounds ◽  
Further Development ◽  
Derivatives Of

New derivatives of licochalcone A were synthesized and evaluated for their potential anticancer activities. Compounds 6 (( E)-N-(4-(3-(5-bromo-4-hydroxy-2-methoxy phenyl) acryloyl) phenyl)-4-isopropylbenzamide) and 8 (1-(3-dimethylamino-phenyl)-3-(2-trifluoromethyl-phenyl)-propenone) showed potent activity against the screened cancer cell lines with that of compound 6 ranging from 6.9 ± 0.2 μM to 22.9 ± 3.1 μM, and that of compound 8 from 4.2 ± 0.5 μM to 11.8 ± 0.7 μM. Both compounds showed stronger cytotoxicity than that of licochalcone A. These two candidates have very different substituents and could be considered as promising lead compounds for further development of potent anticancer agents.

scholarly journals Syntheses and Anticancer Activities of Novel Glucosylated (-)-Epigallocatechin-3-Gallate Derivatives Linked via Triazole Rings

2021 ◽  
Author(s):  
Cheng-Ting Zi ◽  
Bo-Ya Shi ◽  
Ze-Hao Wang ◽  
Ning Zhang ◽  
Yin-Rong Xie ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Anticancer Activities ◽  
Glucose Residue ◽  
Human Cancer Cell Lines ◽  
Mtt Assays ◽  
Mcf 7

Abstract Novel glucosylated (-)-epigallocatechin-3-gallate derivatives 10 – 13 having the EGCG analogues conjugated to the D-glucosyl azide were synthesized by carrying out the copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction, and were evaluated for their cytotoxicities against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using MTT assays. Compounds 10 and 11 showed the highest levels of cytotoxicity against the HL-60 cells with IC50 values of 4.57 μM and 3.78 μM, respectively, and showed moderate selectivity towards cancer cell lines. Compound 11 was also shown to induce apoptosis in HL-60 cells. Most notably, inclusion of the perbutyrylated glucose residue in an EGCG derivative was concluded to lead to increased anticancer activity.

Novel Pyrazolyl Benzoxazole Conjugates: Design, Synthesis, Molecular Docking Studies and in vitro Anticancer Activities

2019 ◽  
Vol 16 (8) ◽  
pp. 619-626
Author(s):  
Arunkumar Thiriveedhi ◽  
Ratnakaram Venkata Nadh ◽  
Navuluri Srinivasu ◽  
Narayana Murthy Ganta
Keyword(s):  
Molecular Docking ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Docking Studies ◽  
Anticancer Activities ◽  
Molecular Docking Studies ◽  
Hybrid Molecules ◽  
Mcf 7

Nowadays, hybrid drugs have gained a significant role in the treatment of different health problems. Most of the hybrid molecules with different heterocyclic moieties were proved to be potent anti-tumor agents in cancer chemotherapy. Hence, the present study is aimed at the evaluation of in vitro anticancer activity of novel hybrid molecules (pyrazolyl benzoxazole conjugates) and to investigate their anticancer activity by molecular docking studies. Designed, synthesized and characterized the novel pyrazolyl benzoxazole conjugates. Anticancer activity of these compounds was determined by SRB assay. Then molecular docking studies were carried out against proto-oncogene tyrosine-protein kinase (ATP-Src, PDB: 2BDF), a putative target for cancer. All the synthesized compound derivatives were evaluated against MCF-7, KB, Hop62 and A549 cancer cell lines. Compounds 9b and 9c exhibited excellent anticancer activities with GI50 values of <0.1 µM against MCF-7 and A549 cell lines. Compound 9e exhibited good antitumor activity on MCF-7 and A-549 with GI50 values of 0.12 µM and 0.19 µM respectively. Compound 9g showed better anticancer activity on A-549 cancer cell line with GI50 of 0.34 µM. The two-hybrid molecules 9b and 9c are found to be comparably potent with the standard drug doxorubicin and may act as drug lead compounds in medicinal chemistry aspect. The present docking investigation proved that having benzoxazole of compound 9c at the position of benzofuran of reference compound (N-acetyl pyrazoline derivative) might be valid for contributing to anti-cancer activity.

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