Synthesis and screening method and kit for lead compound

Abstract

The present invention discloses a synthesis and screening method for a lead compound. The synthesis and screening method comprises: (1) taking raw materials: taking i synthesis blocks and (i+2) single-stranded DNA fragments; (2) adopting a combination chemical method to synthesize compounds so as to obtain a library of the single-stranded DNA-labeled compounds; (3) screening: screening on the library of the DNA-labeled compounds; and (4) sequencing: taking the DNA-labeled compound screened in the step (3), sequencing the DNA on the DNA-labeled compound, and determining the synthesis block and the reaction process of the compound according to the DNA sequence. The invention further discloses a synthesis and screening kit for a lead compound, and a combination chemical library. With the method and the kit, the target lead compound can be quickly and efficiently synthesized and screened, the operations are simple, and the cost is low.

Description

technical field [0001] The invention relates to the field of chemistry, in particular to a synthesis and screening method and kit of a lead compound. Background technique [0002] Since the late 1980s, with the breakthrough of molecular biology research - the development of high-throughput screening technology, the number of new molecular entities required for the development of new drugs has increased, and scientists have shifted their attention from searching for natural products to synthetic large ones. A large number of compound groups - chemical library, chemical library is composed of many organic compounds with different properties. Combinatorial chemistry is a technique for synthesizing chemical libraries in which different series of synthetic building blocks—reactive components—are ordered to form a large series of diverse molecular entity groups. Combinatorial chemical synthesis is often referred to as a number game, that is, how to arrange a large number of synth...

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Problems solved by technology

[0007] However, when double-stranded DNA is used to mark synthetic building blocks or compounds, the double-stranded DNA is easily cross-linked during the ligation extension process to form a coiled tertiary structure. During sequencing, it needs to be melted, and the operation is more complicated. Double-stranded DNA is used to mark When there are more than three steps of linear combination reactions, the sequencing results of double-stranded DNA have large errors, so that the method can only stay in two dimensions, so the number of compounds in the library can only be increased by increasing the number of synthetic building blocks in each step of the reaction. The obtained compound library has poor diversity, and it is difficult to synthesize the target compound

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