SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL PYRAZOLO[3,4-D]PYRIMIDINE DERIVATIVES OF EXPECTED ANTICANCER ACTIVITY

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC50＞79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC50=65.3μM), it indeed significantly abrogated endothelia cell migration (IC50=6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.

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Synthesis and biological evaluation of 4-substituted aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione as anti-cancer and anti-angiogenesis agents

10.21203/rs.2.19336/v3 ◽

2020 ◽

Author(s):

Lifang Guo ◽

Benshan Xu ◽

Zirui Wan ◽

Lulu Ren ◽

Jie Zhang ◽

...

Keyword(s):

Biological Evaluation ◽

Cytotoxic Activities ◽

H Nmr ◽

Chemical Structures ◽

Piperazine Derivatives ◽

Anti Cancer ◽

And Migration ◽

Anti Tumor Activity ◽

Synthesis And Biological Evaluation ◽

Derivatives Of

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.0 2,6 ] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1 H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC 50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC 50 ＞ 79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC 50 =65.3μM), it indeed significantly abrogated endothelia cell migration (IC 50 =6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.

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Synthesis and Biological Evaluation of Novel 4-Phenylaminobenzofuro[2,3-d]pyrimidine Derivatives

Journal of the chemical society of pakistan ◽

10.52568/000659 ◽

2020 ◽

Vol 42 (4) ◽

pp. 564-564

Author(s):

Ju liu Ju liu ◽

Jun Li Jun Li ◽

Jian tao Shi Jian tao Shi ◽

Jie Li Jie Li ◽

Xue chen Hao Xue chen Hao ◽

...

Keyword(s):

Cell Lines ◽

A549 Cells ◽

Positive Control ◽

Biological Evaluation ◽

Dependent Manner ◽

Pyrimidine Derivatives ◽

Concentration Dependent Manner ◽

Ic50 Value ◽

Synthesis And Biological Evaluation

A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.

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