Diagnosis and treatment integrated antitumor drug Caba-808 and preparation method thereof

Abstract

The invention discloses a diagnosis and treatment integrated antitumor drug Caba-808 and a preparation method thereof, the structural formula of the Caba-808 is as shown in formula I as shown in the description, wherein R1 is any one of -H, -CH3 or -CH3CO, and R1 is any one of -C6H5, -NHCOC6H5 or -NHCOOC(CH3)3. The anti-tumor drug Caba-808 provided by the invention can be combined with tubulin to inhibit mitosis of cells, so that an anti-tumor effect is achieved. Meanwhile, the drug has a good fluorescence imaging effect in a near-infrared region, and can clearly display the part and size of a tumor. On the other hand, the preparation method of the novel anti-tumor medicine is simple and easy to operate, and the production cost can be effectively reduced to realize industrial production.

Description

technical field [0001] The invention belongs to the field of synthesizing antitumor drugs integrated with diagnosis and treatment, and in particular relates to an antitumor drug Caba-808 integrated with diagnosis and treatment, and also relates to a preparation method of the above-mentioned medicine. Background technique [0002] Urothelial carcinoma of the bladder is the most common malignant tumor of the urinary system in my country. Most bladder cancer patients are muscle non-invasive bladder cancer, but about 20% of new cases have muscle invasion at the time of initial diagnosis, about 5% of patients have distant metastasis at the time of diagnosis, and about 50% of patients with muscle-invasive bladder cancer will experience local recurrence and distant metastasis. For these patients, local surgical treatment cannot be completely cured. For patients with muscle-invasive bladder cancer, they often rely on cytotoxic drug chemotherapy, but the treatment Methods The tumor ...

AI Technical Summary

Problems solved by technology

Most bladder cancer patients are muscle non-invasive bladder cancer, but about 20% of new cases have muscle invasion at the time of initial diagnosis, about 5% of patients have distant metastasis at the time of diagnosis, and about 50% of patients with muscle-invasive bladder cancer will experience local recurrence and distant metastasis. For these patients, local surgical treatment cannot be completely cured. For patients with muscle-invasive bladder cancer, they often rely on cytotoxic drug chemotherapy, but the treatment Methods The tumor response rate is low, and the adverse reactions are high, the patient tolerance is poor, and the final patient often dies from the distant metastasis of the tumor

[0003] Kidney cancer is also one of the most common malignant tumors of the urinary system. There are more than 60,000 new cases of kidney cancer each year in my country, and more than 20,000 deaths due to kidney cancer. Hematuria, low back pain, and abdominal mass are the most common clinical symptoms of kidney cancer. However, less than 10% of patients have clinical symptoms. Surgical treatment is the best way to treat kidney cancer. However, due to its insidious onset, about 30% of patients have metastasized at the time of diagnosis, and the best time for treatment has been lost.

In addition, different from foreign countries, only about 30% of new cases in my country are localized prostate cancer, while the rest of the new cases are locally advanced or metastatic prostate cancer. These patients miss the chance of radical treatment and need After receiving anti-androgen therapy, but after a median of 18 months of anti-androgen therapy, patients tend to develop castration-resistant prostate cancer, which is highly resistant to drugs, and about 1 / 3 of prostate cancer Patient dies from metastatic castration-resistant prostate cancer

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