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本文引用的文献

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Discovery of Novel Bicyclic Phenylselenyl-Containing Hybrids: An Orally Bioavailable, Potential, and Multiacting Class of Estrogen Receptor Modulators against Endocrine-Resistant Breast Cancer.新型双环苯硒基杂合体的发现:一类口服生物利用度高、具有多效作用的雌激素受体调节剂,可用于治疗内分泌抵抗型乳腺癌。
J Med Chem. 2022 Jun 9;65(11):7993-8010. doi: 10.1021/acs.jmedchem.2c00525. Epub 2022 May 24.
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Diastereoselective approach to rationally design tetrahydro-β-carboline-isatin conjugates as potential SERMs against breast cancer.用于合理设计四氢-β-咔啉-异吲哚酮缀合物作为抗乳腺癌潜在选择性雌激素受体调节剂的非对映选择性方法。
RSC Adv. 2019 Mar 28;9(17):9809-9819. doi: 10.1039/c9ra00744j. eCollection 2019 Mar 22.
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Synthesis and anti-proliferative evaluation of naphthalimide-chalcone/pyrazoline conjugates as potential SERMs with computational validation.萘酰亚胺-查尔酮/吡唑啉共轭物作为潜在选择性雌激素受体调节剂的合成、抗增殖评估及计算验证
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Gefitinib-Tamoxifen Hybrid Ligands as Potent Agents against Triple-Negative Breast Cancer.吉非替尼-他莫昔芬杂合配体作为抗三阴性乳腺癌的有效药物
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Immunotherapy for early triple negative breast cancer: research agenda for the next decade.早期三阴性乳腺癌的免疫治疗:未来十年的研究议程。
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分子杂合体在乳腺癌研究与治疗中的治疗意义。

Therapeutic significance of molecular hybrids for breast cancer research and treatment.

作者信息

Ahmad Irshad

机构信息

Department of Mathematics and Natural Sciences, School of Arts and Sciences, American University of Ras Al Khaimah Ras Al Khaimah United Arab Emirates

出版信息

RSC Med Chem. 2022 Nov 29;14(2):218-238. doi: 10.1039/d2md00356b. eCollection 2023 Feb 22.

DOI:10.1039/d2md00356b
PMID:36846377
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9945856/
Abstract

Worldwide, breast cancer is still a leading cause of cancer death in women. Indeed, over the years, several anti-breast cancer drugs have been developed; however, the complex heterogeneous nature of breast cancer disease reduces the applicability of conventional targeted therapies with the upsurge in side effects and multi-drug resistance. Molecular hybrids generated by a combination of two or more active pharmacophores emerged as a promising approach in recent years for the design and synthesis of anti-breast cancer drugs. The hybrid anti-breast cancer molecules are well known for their several advantages compared to the parent moiety. These hybrid forms of anti-breast cancer molecules demonstrated remarkable effects in blocking different pathways contributing to the pathogenies of breast cancer and improved specificity. In addition, these hybrids are patient compliant with reduced side effects and multi-drug resistance. The literature revealed that molecular hybrids are applied to discover and develop novel hybrids for various complex diseases. This review article highlights the recent progress (∼2018-2022) in developing molecular hybrids, including linked, merged, and fused hybrids, as promising anti-breast cancer agents. Furthermore, their design principles, biological potential, and future perspective are discussed. The provided information will lead to the development of novel anti-breast cancer hybrids with excellent pharmacological profiles in the future.

摘要

在全球范围内,乳腺癌仍是女性癌症死亡的主要原因。事实上,多年来已经研发出了几种抗乳腺癌药物;然而,乳腺癌疾病复杂的异质性降低了传统靶向治疗的适用性,副作用增加且出现了多药耐药性。近年来,由两种或更多活性药效基团组合而成的分子杂化物成为抗乳腺癌药物设计与合成的一种有前景的方法。与母体部分相比,杂化抗乳腺癌分子因其诸多优点而广为人知。这些杂化形式的抗乳腺癌分子在阻断导致乳腺癌发病的不同途径以及提高特异性方面显示出显著效果。此外,这些杂化物患者耐受性良好,副作用和多药耐药性降低。文献表明,分子杂化物被用于发现和开发针对各种复杂疾病的新型杂化物。这篇综述文章重点介绍了在开发分子杂化物(包括连接型、融合型和嵌合型杂化物)作为有前景的抗乳腺癌药物方面的最新进展(约2018 - 2022年)。此外,还讨论了它们的设计原则、生物学潜力和未来前景。所提供的信息将有助于未来开发出具有优异药理学特性的新型抗乳腺癌杂化物。