高等学校化学学报

高等学校化学学报 ›› 1998, Vol. 19 ›› Issue (S1): 240.

• Organic Synthesis Chemistry • 上一篇    下一篇

SYNTHESIS OF PORPHYRIN NITROGEN MUSTARDS AND THEIR ANTI-TUMOR ACTIVITIES

Zhi-Long Chen, Jin-Rong Chen, Wei-Qin Wan, De-Yu Xu   

  1. Institute of Pharmaceutical Chemistry, Second Military Medical University, 800 Xiang Yin Road, Shanghai 200433
  • 出版日期:1998-12-31 发布日期:1998-12-31

SYNTHESIS OF PORPHYRIN NITROGEN MUSTARDS AND THEIR ANTI-TUMOR ACTIVITIES

Zhi-Long Chen, Jin-Rong Chen, Wei-Qin Wan, De-Yu Xu   

  1. Institute of Pharmaceutical Chemistry, Second Military Medical University, 800 Xiang Yin Road, Shanghai 200433
  • Online:1998-12-31 Published:1998-12-31

PDF (PC)

摘要： With the development of laser medicine and technology in light-conducted fiber and endoscope, photodynamic therapy (PDT) obtained regulatory approvals in the United States and elsewhere to cure malignent tumors in skin, esophagi, bronchi and bladder for it's selective tumoricidal effects without the serious side effects of conventional therapy in a variety of tumors. We focused our attention on both the alleviation of patient's suffering from damages of normal tissues in chemotherapy and the eliminating of cutaneous photosensitivity as well as the enhancement of the depth of tumor necrosis which is generally not more than 8-10 nm even under the maximum safe light dose in PDT. Thus, a series of new compounds porphyrin nitrogen mustards, namely, 2,7,12,18-tetramethyl-13,17,di[3-N,N-di(2-chloroethyl) amino propyl] porphin (I1) and 2,7,12,18-tetramethyl-3,8-di(l-alkyloxyethyl)-13,17-bis[3-N, N-di(2-chloroethyl)amino propyl]porphin (I2-8) were synthesized(I) by introducing the alkylating agent nitrogen mustard into the periphery of porphyrin(Scheme 1). The mean overall yield of I2-8 is 13%.

Abstract: With the development of laser medicine and technology in light-conducted fiber and endoscope, photodynamic therapy (PDT) obtained regulatory approvals in the United States and elsewhere to cure malignent tumors in skin, esophagi, bronchi and bladder for it's selective tumoricidal effects without the serious side effects of conventional therapy in a variety of tumors. We focused our attention on both the alleviation of patient's suffering from damages of normal tissues in chemotherapy and the eliminating of cutaneous photosensitivity as well as the enhancement of the depth of tumor necrosis which is generally not more than 8-10 nm even under the maximum safe light dose in PDT. Thus, a series of new compounds porphyrin nitrogen mustards, namely, 2,7,12,18-tetramethyl-13,17,di[3-N,N-di(2-chloroethyl) amino propyl] porphin (I1) and 2,7,12,18-tetramethyl-3,8-di(l-alkyloxyethyl)-13,17-bis[3-N, N-di(2-chloroethyl)amino propyl]porphin (I2-8) were synthesized(I) by introducing the alkylating agent nitrogen mustard into the periphery of porphyrin(Scheme 1). The mean overall yield of I2-8 is 13%.

TrendMD: