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anticancer conjugates
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A technology of drug conjugates and drugs, applied in drug combinations, antitumor drugs, organic active ingredients, etc., can solve the problems of inability to act on cancer cells, poor targeting, and affecting the performance of normal cells.
Active Publication Date: 2021-01-05
BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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However, the drug still has disadvantages. For example, it has poor targeting and cannot act on specific cancer cells. While killing cancer cells, it will also affect the performance of normal cells, so that the incidence of adverse reactions is still relatively high.
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Embodiment 1
[0124]
[0125] Preparation of compound 2
[0126] Add 3.50g of compound 1 (1.0eq) and 52.5ml of DMF to a 250mL round bottom flask, heat to 60°C to dissolve, evaporate the DMF under reduced pressure after 5-10min, add 300ml of n-heptane and distill under reduced pressure, repeat three times, spin dry Add 105ml of DCM, 1.08g of Boc-Gly-OH (1.2eq), 63mg of DMAP (0.1eq), add dropwise a solution of 1.59g of DCC (1.5eq) dissolved in 10ml of DCM, and react at 20°C for 4 hours. After the reaction is monitored by TLC, filter and concentrate When the remaining 25% volume was reached, 120ml of IPA was added, 75% of the solvent was evaporated, 150ml of n-heptane was added, stirred at room temperature for 1 hour, filtered, washed twice with n-heptane, and dried to obtain 4.02g of compound 2 as a pale yellow solid.
[0127] Preparation of compound 3
[0128] Add 4.02g of compound 2 and 50ml of DCM to a 100mL three-neck flask, stir and dissolve, then add 11.6ml of TFA dropwise, react at...
Embodiment 2
[0130]
[0131] Preparation of compound 5
[0132] Add 6.9g of compound 4 and 30ml of EA into a 250mL three-neck flask, stir to dissolve and cool down to 0°C, add 40ml of 0.3M HCl / EA, keep the reaction for 2h, monitor the reaction by TLC and concentrate to dryness to obtain compound 5, directly proceed to the following One step reaction.
[0133] Preparation of Compound 6
[0134] Dissolve compound 5 (1.0eq) with 50ml of purified water, add 3.96g of sodiumbicarbonate (2.0eq), dissolve 5.30g of Fmoc-OSU (1.0eq) with 50ml of DME, add it to the reaction flask of compound 5, and add 25ml of THF , stirred at room temperature for 2 hours, after the reaction was monitored by TLC, evaporated the organic solvent, extracted impurities with EA, adjusted the pH of the aqueous phase to 3-4 with dilute hydrochloric acid, extracted twice with EA, combined the organic phases, washed once with water, and washed with saturated saline It was dried over anhydroussodiumsulfate and concentr...
Embodiment 3
[0140] Preparation of Targeting Molecule GE11 (Compound 60) Linked with Protecting Group
[0141]
[0142] The sequence of GE11 is YHWYGYTPQNVI
[0143] Using 2Cl-Trt Resin, using HOBT / DIC as the couplingreagent, DMF as the reaction solvent, and using ninhydrin detection method for reaction monitoring, the following protected amino acids were connected to the resin in sequence: Fmoc-Ile-OH, Fmoc-Val-OH, Fmoc-Asn(Trt)-OH, Fmoc-Gln(Trt)-OH, Fmoc-Pro-OH, Fmoc-Thr(tBu)-OH, Fmoc-Tyr(tBu)-OH, Fmoc-Gly-OH, Fmoc- Tyr(tBu)-OH, Fmoc-Trp(Boc)-OH, Fmoc-His(Trt)-OH, Boc-Tyr(tBu)-OH, add cleavage reagent: acetic acid / TFE / DCM=1 / 2 / 7, After reacting for 2 hours, ice-based MTBE was precipitated, washed, and dried to obtain 60 as an off-white solid.
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Abstract
The invention discloses a multibranched drug conjugate or pharmaceutically acceptable salts thereof, wherein the multibranched drug conjugate has a structural formula shown as (I). The formula is shown in the description. R is an organic center, POLY is a polymer, L is a multivalent junction, T is a targeting molecule, D is an active agent, q is any integer between 3 and 8, wherein the formula ofL is shown in the description. The symbol * represents a linking point between the multivalent junction L and the target molecule T, # represents a linking point between the multivalent junction L andthe active agent D, and % represents a linking point between the multivalent junction L and the POLY; l is any integer between 2 and 20, m and n are respectively any integer between 0 and 10, T is GE11 and D is a camptothecindrug. The conjugate disclosed by the invention, compared with small molecule anticancer compounds, has higher inhibiting ability to tumors and is suitable for solid tumor types such as colon cancer, breast cancer, ovarian cancer, pancreatic cancer, gastric cancer, glioma, malignant sarcoma of breast, ovary, colon, kidney, bile duct, lung and brain as well as cancer and lymphoma.
Description
technical field [0001] The invention relates to a multi-arm polymer modified targeting anticancer conjugate, more specifically, the invention relates to linking a targeting molecule with an anticancer drug through a multi-arm polymer to form a conjugate. Background technique [0002] Over the years, various approaches have been proposed for improving the stability and delivery of bioactive agents. Challenges associated with the formulation and delivery of pharmaceutical agents can include poor aqueous solubility, toxicity, low bioavailability, instability, and rapid in vivo degradation of the pharmaceutical agent. Although many approaches have been devised to improve the delivery of pharmaceutical agents, no single approach is without its drawbacks. For example, commonly used drug delivery methods aim to solve or at least improve one or more of the following problems, including drug encapsulation, covalent attachment, etc., in a liposome, polymer matrix, or unimolecular mic...
Claims
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Application Information
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