Synthesis and antitumor activity of ureas containing pyrimidinyl group

Jin, Chuanfei; Liang, Yong; He, Hongwu; Fu, Liwu

doi:10.1016/j.ejmech.2010.11.026

Cited by 32 publications

(12 citation statements)

References 13 publications

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“…Consequently, there is an urgent need for the implementation of efficient prevention and treatment strategies to curb cancer deaths. Investigating small molecule antitumor agents, which could decrease drug resistance and reduce unpleasant side effect is more desirable [5].…”

Section: Introductionmentioning

confidence: 99%

“…CYC116, Cyclacel (4) was an effective Aurora A/B inhibitor and a slightly weaker inhibitor of VEGFR2 and was currently in Phase I clinical trials [21]. Dasatinib (5), a novel, highly potent, and multitargeted inhibitor of Abl, Src, and c-Kit kinase, which was potent against unmutated BCR-ABL [22], was recently approved for the oral treatment of CML and Philadelphia chromosome-positive acute lymphoblastic leukemia [23].…”

Section: Introductionmentioning

confidence: 99%

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Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

Alizadeh

Hashemi

2021

Med Chem Res

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Currently, the development of anticancer drug resistance is significantly restricted the clinical efficacy of the most commonly prescribed anticancer drug. Malignant disease is widely prevalent and considered to be the major challenges of this century, which concerns the medical community all over the world. Consequently, investigating small molecule antitumor agents, which could decrease drug resistance and reduce unpleasant side effect is more desirable. 2-aminothiazole scaffold has emerged as a promising scaffold in medicinal chemistry and drug discovery research. This nucleus is a fundamental part of some clinically applied anticancer drugs such as dasatinib and alpelisib. Literature survey documented that different 2aminothiazole analogs exhibited their potent and selective nanomolar inhibitory activity against a wide range of human cancerous cell lines such as breast, leukemia, lung, colon, CNS, melanoma, ovarian, renal, and prostate. In this paper, we have reviewed the progresses and structural modification of 2-aminothiazole to pursuit potent anticancers and also highlighted in vitro activities and in silico studies. The information will useful for future innovation.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

Alizadeh

Hashemi

2021

Med Chem Res

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“…Among all the current therapeutic methods, chemotherapy still remains an important option for cancer treatment. [1][2][3] However, the major hindrance to successful cancer chemotherapy is the development of drug and multidrug-resistance, in which cancer cells become simultaneously resistant to different structural types of chemotherapeutic agents and the development of novel anticancer drug. [4][5][6] Therefore, there is a need of new approaches that are specifically designed to avoid these drawbacks.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Novel Benzamide- piperazine-sulfonamide Hybrids as Potential Anticancer Agents

Rao

Katiki

Dileep

et al. 2019

Croat. chem. acta (Online)

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The synthesis of a series of substituted hippuric acid (2-benzamidoacetic acid) derivatives containing arylsulfonylpiperazine nucleus (3a–j, 4a–j) is described. The compounds were synthesized by coupling hippuric/4-fluorohippuric acid with various arylsulfonylpiperazines using N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (EDCI). The structures of all the new compounds were confirmed by IR, NMR and MS spectral data. All the synthesized compounds have been evaluated for their in vitro cytotoxicity towards five human cancer cell lines of different origins viz. HeLa (Cervical), A549 (Lung), A375 (Skin), MD-AMB-231(Breast) and T98G (brain) and their IC50 values were determined. Among the compounds tested, 3b, 3d, 3g, 4c and 4e displayed significant cytotoxic activity (IC50 = 24.2–38.2 µM). T98G was the most sensitive cell line towards the compounds studied followed by HeLa, A375, A549 and MD-AMB-231.

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“…Although there has been huge progress in the treatment of cancer, the fruitful treatment of cancer remains a challenge to the public health and scientific communities worldwide. Hence, development of safer anticancer agents with broader spectrum of cytotoxicity to tumor cells is felt to be the need of the hour . In this context in the past few decades, various research groups focused on the synthesis and chemical modification of naturally occurring compounds.…”

Section: Introductionmentioning

confidence: 99%

Molecular Engineering of Tetracyclic 2,3‐Dihydro‐1H‐benzo[2,3]‐benzofuro[4,5‐e][1,3]oxazine Derivatives: Evaluation for Potential Anticancer Agents

Botla

Pilli

Koude

et al. 2017

Archiv der Pharmazie

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Water-mediated one-pot Mannich type condensation of dibenzo[b,d]furan-2-ol with different amines resulted in a large library of novel 2,3-dihydro-1H-benzo[2,3]benzofuro[4,5-e][1,3]oxazine derivatives in moderate to excellent yields. The ortho-aminomethylation of the dibenzofuranols proceeded smoothly in the presence of various aromatic/aliphatic amines and paraformaldehyde, followed by cyclization. All the newly synthesized tetracyclic 2,3-dihydro-1H-benzo[2,3]benzofuro[4,5-e][1,3]oxazine derivatives were chemically characterized and screened for their cytotoxicity activity by cell viability assay (MTT test) against three human cancer cell lines and antibacterial activity by determining the minimum inhibitory concentration (MIC) against four bacterial strains. Among all the derivatives, MCV-24 showed promising anticancer activity by inhibiting the cell proliferation of an ovarian cancer cell line (SKOV3) with an IC value at 7.5 µM, whereas MCV-24 to MCV-30 derivatives showed moderate activity against a lung cancer cell line (A549) with an IC value ranging from 11 to 15.9 µM. Besides MCV-29, -30, and -31 also exhibited broad-spectrum antibacterial activity. Among all new compounds, MCV-24-30 showed promising anticancer and MCV-29-31 antibacterial activity.

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Synthesis and antitumor activity of ureas containing pyrimidinyl group

Cited by 32 publications

References 13 publications

Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

Synthesis of Novel Benzamide- piperazine-sulfonamide Hybrids as Potential Anticancer Agents

Molecular Engineering of Tetracyclic 2,3‐Dihydro‐1H‐benzo[2,3]‐benzofuro[4,5‐e][1,3]oxazine Derivatives: Evaluation for Potential Anticancer Agents

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