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Exploring the Synthesis and Anticancer Potential of L-tyrosine-platinum(II) Hybrid Molecules

机译：L-酪氨酸-铂（II）杂化分子的合成及抗癌潜力的探讨

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摘要

The search for new specific chemotherapeutic drugs designed to minimize the toxic side effects resulting from chemotherapy is still a subject of intense research. The objective of the current study was to design a non-steroidal-platinum(II) derivative that would target the estrogen receptor alpha (ER alpha) without triggering estrogenic cell proliferation. For this purpose, the amino acid L-tyrosine was modified and attached to a cisplatin analog. Hence, the L-tyrosine portion of the molecule could possibly act as a transporter to target the ER alpha protein and, by doing so concentrate the cytotoxic moiety to hormone-dependent breast cancer cells. Herein, we describe three different alternative methodologies that were used to make these new anticancer molecules. The L-tyrosine-Pt(II) hybrid 5b was made in four steps with 36% overall yield by the first method, in six steps with 11% overall yield by the second method and, in four steps with 23% overall yield by the third method. Preliminary biological activity on breast cancer cell lines indicated that the final hybrids (5a and 5b) were unfortunately inactive but their platinum(II) precursors (14a and 14b) showed activity similar to that of cisplatin.
机译：寻找新的特定化学治疗药物以最大程度地减少化学疗法产生的毒副作用仍然是一项深入研究的课题。当前研究的目的是设计一种非甾体铂（II）衍生物，该衍生物将靶向雌激素受体α（ER alpha）而不会触发雌激素细胞增殖。为此目的，氨基酸L-酪氨酸被修饰并连接至顺铂类似物。因此，该分子的L-酪氨酸部分可能充当靶向ERα蛋白的转运蛋白，并因此将细胞毒性部分集中于激素依赖性乳腺癌细胞。在本文中，我们描述了用于制造这些新抗癌分子的三种不同的替代方法。通过第一种方法分四个步骤生产L-酪氨酸-Pt（II）杂化物5b，通过第二种方法分六个步骤生产L-酪氨酸-Pt（II）杂物，总产率为11％，通过分四步生产L-酪氨酸-Pt（II）杂化物5b第三种方法。对乳腺癌细胞系的初步生物学活性表明，不幸的是最终的杂种（5a和5b）没有活性，但它们的铂（II）前体（14a和14b）显示出与顺铂相似的活性。

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