Web通过研究我们发现牛蒡子苷元抗肿瘤机制是它能够有效地抑制葡萄糖缺乏肿瘤细胞的能量代谢，从而造成肿瘤细胞坏死。. 于是，我们选择了牛蒡子苷元为先导化合物，合成了一系列的牛蒡子苷元的类似物，包括：酯类、醚类、曼尼希碱类以及4-氨基-4-去羟基类 ... Web1 Feb 2005 · Bioisosterism is a strategy of Medicinal Chemistry for the rational design of new drugs, applied with a lead compound (LC) as a special process of molecular …

Bioisostere - an overview ScienceDirect Topics

WebDefinition of Bioisosterism Friedman (1951): Bioisosteresare atoms or molecules that fit the broadest definition for isosteresand have the same type of biological activity. Thornber(1979): Groups or molecules which have chemical and physical similarities producing broadly similar biological effects. Parameters affected with … Web3 Feb 2024 · Bioisosteric replacement is a powerful tool for modulating the drug-like properties, toxicity, and chemical space of experimental therapeutics. In this review, we focus on selected cases where bioisosteric replacement and scaffold hopping have been used in the development of new anti-HIV-1 therapeutics. Moreover, we cover field-based, … if one were to say

1,2,4-Triazolo[4,3-c]quinazolines: a bioisosterism-guided approach ...

Web生物电子等排（Bioisosterism）是由早期的电子等排（Isosteriam）发展和延伸来的。 早在1919年Langmuir就在无机化学中提出了电子等排体（Isostere）的概念，即凡是具 . 有相同数目的原子和电子，并且电子排列状况也相同的分子、原子或基团（离子）称为电 . 子等排体 ... WebIn medicinal chemistry, bioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological properties to … In medicinal chemistry, bioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological properties in the same chemical compound. In drug design, the purpose of exchanging one bioisostere for another is to enhance … See more Classical bioisosteres Classical bioisosterism was originally formulated by James Moir and refined by Irving Langmuir as a response to the observation that different atoms with the same See more • Grimm's hydride displacement law, an early hypothesis to describe bioisosterism See more Bioisosteres of some patented compounds can be discovered automatically and used to circumvent Markush structure patent claims. It has been proposed that key force field features, that is the pharmacophore, be patented instead. See more if one won\\u0027t another one will